- Design, green synthesis, molecular docking and anticancer evaluations of diazepam bearing sulfonamide moieties as VEGFR-2 inhibitors
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Novel series of diazepam bearing sulfonamide moieties 5a-f and 7a-c were designed, synthesized and evaluated for anticancer activity against HepG2, HCT-116 and MCF-7 cell lines. MCF-7 was the most sensitive cell line to the influence
- Saleh, Nashwa M.,El-Gaby, Mohamed S.A.,El‐Adl, Khaled,Abd El-Sattar, Nour E.A.
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- Intra- and intermolecular hydrogen bonding and conformation in 1-acyl thioureas: An experimental and theoretical approach on 1-(2-chlorobenzoyl)thiourea
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The vibrational analysis (FT-IR and FT-Raman) for the new 1-(2-chlorobenzoyl)thiourea species suggests that strong intramolecular interactions affect the conformational properties. The X-ray structure determination corroborates that an intramolecular N-H?OC hydrogen bond occurs between the carbonyl (-CO) and thioamide (-NH2) groups. Moreover, periodic system electron density and topological analysis have been applied to characterize the intermolecular interactions in the crystal. Extended N-H?SC hydrogen-bonding networks between both the thioamide (N-H) and carbamide (NH2) groups and the thiocarbonyl bond (CS) determine the crystal packing. The Natural Bond Orbital (NBO) population analysis demonstrates that strong hyperconjugative remote interactions are responsible for both, intra and intermolecular interactions. The Atom in Molecule (AIM) results also show that the N-H?Cl intramolecular hydrogen bond between the 2-Cl-phenyl ring and the amide group characterized in the free molecule changes to an N?Cl interaction as a consequence of crystal packing.
- Saeed, Aamer,Khurshid, Asma,Bolte, Michael,Fantoni, Adolfo C.,Erben, Mauricio F.
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- Synthesis, characterization, X-ray crystal structure, DFT calculation and antibacterial activities of new vanadium(IV, V) complexes containing chelidamic acid and novel thiourea derivatives
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Three new thiourea ligands derived from the condensation of aroyl- and aryl-isothiocyanate derivatives with 2,6-diaminopyridine, named 1,1′-(pyridine-2,6-diyl)bis(3-(benzoyl)thiourea) (L1), 1,1′-(pyridine-2,6-diyl)bis(3-(2-chlorobenzoyl)thiourea) (L2) and
- Farzanfar, Javad,Ghasemi, Khaled,Rezvani, Ali Reza,Delarami, Hojat Samareh,Ebrahimi, Ali,Hosseinpoor, Hona,Eskandari, Amir,Rudbari, Hadi Amiri,Bruno, Giuseppe
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- Straightforward synthesis of 2-chloro-N-(5-(cyanomethyl)-1,3,4-thiadiazol-2-yl)benzamide as a precursor for synthesis of novel heterocyclic compounds with insecticidal activity
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The current work is devoted to the synthesis of 2-chloro-N-(5-(cyanomethyl)-1,3,4-thiadiazol-2-yl)benzamide 5 by an efficient synthetic methodology. The authors decided to exploit the reactivity of cyanomethylene functionality to construct new heterocycle
- Mohamed, Ali M. M.,Ismail, Mahmoud F.,Madkour, Hassan M. F.,Aly, Aly Fahmy,Salem, Marwa S.
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- Phase-transfer-catalyzed synthesis of N-aryl-N'-(2-chlorobenzoyl)-thiourea derivatives
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Reaction of aromatic amines with 2-chlorobenzoyl chloride and ammonium thiocyanate under the condition of solid-liquid phase-transfer catalysis using polyethylene glycol-400 (PEG-400) as the catalyst yielded N-aryl-N'-(2-chlorobenzoyl)thioureas 3a-3j in g
- Zhang, Youming,Wei, Taibao,Wang, Lailai
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- Design and synthesis of novel thiourea metal complexes with controllable antibacterial properties
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A new bidentate O,S donor thiourea ligand (L1), namely N-(2-hydroxyethyl)-N′-2-chlorobenzoylthiourea, and its oxazolidine derivative (L2) were synthesized. Derivative L2 was used for the preparation of Ni(L2)2 and Cu(L2)2 complexes. The compounds were investigated using X-ray crystallography and Fourier transform infrared, 1H NMR and UV–visible spectroscopies. Single-crystal X-ray analysis showed strong hydrogen bonding interactions between carbonyl oxygen and N(10) ─ H in the L1 ligand. In addition, the antibacterial activities of these compounds were evaluated against Gram-positive and Gram-negative bacteria, measured using the colony count method. The Cu(L2)2 complex exhibited a significant antibacterial activity while the activity of the other compounds was much lower. Finally, the relationship between the structure and antibacterial properties of these compounds was investigated using highest occupied and lowest unoccupied molecular orbital energies calculated by density functional theory method based on the 6-31G*/LANL2DZ basis set.
- Rakhshani, Sajjad,Rezvani, Ali Reza,Du?ek, Michal,Eigner, Václav
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- Mononuclear copper(i) complexes of triphenylphosphine and: N, N ′-disubstituted thioureas as potential DNA binding chemotherapeutics
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In this work, nine new mixed-ligand complexes with the general formula [CuBr(TPP)2Tu1-9] were synthesized. The copper(i) complexes of triphenylphosphine (TPP) and different N,N′-disubstituted thioureas (Tu) were characterized via spectroscopic techniques including Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectroscopy (1H, 13C, and 31P NMR), and single-crystal X-ray diffraction (SC-XRD). The complexes were synthesized via the direct reaction of bromo(tris(triphenylphosphine)copper(i)) [BrCu(PPh3)3] precursor and thiourea ligand solution under ambient conditions. Complexes 1, 2 and 3 crystallized in a triclinic system with the P1 space group. Each complex is mononuclear, and the copper atom is tetrahedrally attached to two TPP groups through the phosphorous atom, one thiourea molecule through the sulfur atom and one bromine atom. The synthesized compounds were docked with a DNA macromolecule to predict their binding site and it was found that all molecules showed favorable binding to the DNA minor grooves. The DNA interaction studies of the representative complexes demonstrated their efficient DNA binding affinities. Based on the docking and DNA interaction results, complex 7 was found to be the best binder with a docking affinity of 382.2 kJ mol-1 and binding constant of 3.96 × 104 M-1. This compound tends to interact with the minor groove through the bromine atom positioning the side triphenylphosphine rings along the X-axis of the groove while keeping the 1-(2-chlorobenzyl)-3-(3-(trifluoromethyl)phenyl)thiourea ring on the outside.
- Khan, Syed Ishtiaq,Ahmad, Sajjad,Khan, Inayat Ali,Badshah, Amin,Rauf, Muhammad Khawar,Putejo, Jahangir Ali,Siddiq, Muhammad Nasir,Kausar, Samia,Altaf, Ataf Ali
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p. 8925 - 8935
(2021/06/01)
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- Synthesis, kinetics and biological assay of some novel aryl bis-thioureas: A potential drug candidates for Alzheimer's disease
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A new series of bis-thioureas (4a-4j) was synthesized and characterized through spectroscopic and elemental analysis. The synthesized compounds 4a-4j were subjected to acetylcholinesterase enzyme (AChE) inhibition activity and free radical scavenging activity. The results of AChE inhibition assay were found to be active in inhibiting the target enzyme with different IC50 values. Among all derivatives, the 4 g showed highly potent inhibition potential against AChE enzyme with IC50 value of 0.1761±0.00768 μM, which is several times better than the reference inhibitor neostigmine methylsulfate IC50 2.469±0.069 μM. The initial structure-activity relationship (SAR) of 4 g revealed dual hydrogen bonding ability (donor and acceptor). Moreover, the electronic environment around the aromatic ring also greatly influenced the enzyme inhibition of AChE. To further explore the newly synthesized AChE inhibitors, kinetic studies were carried out to determine the mode of inhibition and it was found to be competitive inhibition. Pharmacokinetic predictions (ADMET parameters) were also evaluated and compounds showed good lead-like potential with little hepatotoxic and no skin-sensitive effects. The molecular docking studies delineated the binding affinity of the ligands with target protein and showed docking scores in the range of -10.3 to -7.6 kcal/mol.
- Abbas, Qamar,Abd-Rabboh, Hisham S. M.,Bahadur, Ali,Channar, Kashif Ali,Channar, Pervaiz Ali,Hassan, Mubashir,Iqbal, Shahid,Khan, Bilal Ahmad,Kim, Jung Min,Lal, Bhajan,Mahesar, Parvez Ali,Nawaz, Muhammad,Rajoka, Muhammad Shahid Riaz,Rashid, S. G.,Raza, Hussain,Saeed, Aamer,Shah, Mazloom,Siyal, Ali Nawaz,Ujan, Rabail
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- Theoretical and experimental verification of molecular properties of novel benzamide derivatives using computational platforms and in vitro antibacterial activity
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A series of N-(benzo[d]oxazol-2-ylcarbamothioyl)-2/4-substituted benzamides were synthesized by the reaction of 2-aminobenzoxazole with apposite benzoyl isothiocyanate. The structure of the newly synthesized compounds was confirmed by chemical tests, elemental (C, H, N, and S), and spectral (IR, 1H NMR, 13C NMR, and mass) analysis. All the synthesized compounds were evaluated experimentally for their antibacterial activity against Gram-positive and Gram-negative bacteria. The test results show moderate to potent antibacterial activity compared to the standard drug. The binding interactions of newly synthesized ligand and protein were correlated using a molecular docking study using a binding pocket of GlcN-6-P synthase. [Figure not available: see fulltext.].
- Wanjari, Poonam M.,Mokale, Santosh N.,Bharati, Avinash V.,Ingle, Vishwas N.
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p. 655 - 663
(2021/01/07)
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- A PROCESS FOR PREPARING 2-CHLORO-N-{[4-(PYRIMIDIN-2-YLSULFAMOYL)PHENYL] CARBAMOTHIOYL} BENZAMIDE AND THE PHARMACEUTICAL UTILITY THEREOF
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Disclosed is a process for preparing 2-chloro-N-{[4-(pyrimidin-2-ylsulfamoyl)phenyl] carbamothioyl} benzamide (compound 2c).
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Page/Page column 8; 9; 11
(2021/07/10)
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- Synthesis and Spectral Characterization of New 2-(5-Aryl-4H-1,2,4-triazol-3-yl)-1H-isoindole-1,3(2H)-dione Derivatives
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Abstract: A series of novel 2-(5-aryl-4H-1,2,4-triazol-3-yl)-1H-isoindole-1,3(2H)-diones were synthesized in three steps. In the first step, treatment of substituted benzoyl chlorides with ammonium thiocyanate gave the corresponding benzoyl isothiocyanate
- Alimi,Hatamjafari,Shiroudi,Pourshamsian,Oliaey
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p. 631 - 637
(2021/06/02)
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- Synthesis and Investigation of the Antibacterial Activity of New Tris-Thiourea Derivatives
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An efficient procedure for the preparation of symmetrical tris-thiourea derivatives (5a – 5h) by means of one-pot condensation reaction between available benzoyl chlorides (1a –1h) with potassium thiocyanate (2) and melamine (4) under reflux conditions is
- Ghorbani, Saghi Shiroud,Montazeri, Naser,Zeydi, Masoud Mohammadi,Ghane, Masood
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- Exploring amantadine derivatives as urease inhibitors: Molecular docking and structure–activity relationship (sar) studies
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This article describes the design and synthesis of a series of novel amantadine-thiourea conjugates (3a–j) as Jack bean urease inhibitors. The synthesized hybrids were assayed for their in vitro urease inhibition. Accordingly, N-(adamantan-1-ylcarbamothio
- Ahmed, Atteeque,Ali, Omar M.,Ashraf, Zaman,Channar, Pervaiz Ali,El-Bahy, Zeinhom M.,Hassan, Mubashir,Khurshid, Asma,Raza, Hussain,Saeed, Aamer,Tehzeeb, Arfa,Ul-Hamid, Anwar
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- Benzoylthioureas: Design, synthesis and antimycobacterial evaluation
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Background: New drugs and strategies to treat tuberculosis (TB) are urgently needed. In this context, thiourea derivatives have a wide range of biological activities, including anti-TB. This fact can be illustrated with the structure of isoxyl, an old anti-TB drug, which has a thiourea as a pharmacophore group. Objective: The aim of this study is to describe the synthesis and the antimycobacterial activity of fifty-nine benzoylthioureas derivatives. Methods: Benzoylthiourea derivatives have been synthesized and evaluated for their activity against Mycobacterium tuberculosis using the MABA assay. After that, a structure-activity relationship study of this series of compounds has been performed. Results and Discussion: Nineteen compounds exhibited antimycobacterial activity between 423.1 and 9.6 μM. In general, we observed that the presence of bromine, chlorine and t-Bu group at the para-position in benzene ring plays an important role in the antitubercular activity of Series A. These substituents were fixed at this position in benzene ring and other groups such as Cl, Br, NO2 and OMe were introduced in the benzoyl ring, leading to the derivatives of Series B. In general, Series B was less cytotoxic than Series A, which indicates that the presence of a substituent at benzoyl ring contributes to an improvement in both antimycobacterial activity and toxicity profiles. Conclusion: Compound 4c could be considered a good prototype to be submitted to further structural modifications in the search for new anti-TB drugs, since it is 1.8 times more active than the first line anti-TB drug ethambutol and 0.65 times less active than isoxyl.
- Abreu, Lethícia O.,Bispo, Marcelle L. F.,Brito, Tiago O.,Gomes, Karen M.,Louren?o, Maria C. S.,Macedo, Fernando,Pereira, Patricia M. L.,Tisher, Cesar A.,Yamada-Ogatta, Sueli F.,de Fátima, ?ngelo
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- Design, Synthesis, and Insecticidal Activity of Novel Doramectin Derivatives Containing Acylurea and Acylthiourea Based on Hydrogen Bonding
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Our recent investigation on the insecticidal activities of several doramectin derivatives preliminarily revealed that the presence of hydrogen bonds at the C4″ position of the molecule with target protein γ-aminobutyric acid (GABA) receptor was crucial for retaining high insecticidal activity. As a continuation of our research work on the development of new insecticides, two series of novel acylurea and acylthiourea doramectin derivatives were designed and synthesized. The bioassay results indicated that the newly synthesized compounds (5o, 5t, and 6t) exhibited higher insecticidal activity against diamondback moth, oriental armyworm, and corn borer than the control compounds doramectin, commercial avermectins, chlorbenzuron, and lead compound 3g in our laboratory. Specifically, compound 5t was identified as the most promising insecticide against diamondback moth, with a final mortality rate of 80.00% at the low concentration of 12.50 mg/L, showing approximately 7.75-fold higher potency than the parent doramectin (LC50 value of 48.1547 mg/L), 6.52-fold higher potency than commercial avermectins (LC50 value of 40.5507 mg/L), and 3.98-fold higher potency than compound 3g (LC50 value of 24.7742 mg/L). Additionally, molecular docking simulations revealed that compound 5t (2.17, 2.20, 2.56, and 2.83 ?) displayed stronger hydrogen-bond action in binding with the GABA receptor, better than that of compound 5o (1.64 and 2.15 ?) and compound 6t (2.20 and 2.31 ?) at the C4″ position. This work demonstrated that these compounds containing hydrogen-bond groups might contribute to the improvement of insecticidal activity and supply certain hints toward structure optimization design for the development of new insecticides.
- Bai, Ping,Cheng, Yao,Lu, Xiaoxia,Yang, Jian,Zhang, Qi,Zheng, Cheng
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p. 5806 - 5815
(2020/06/19)
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- Nano nickel [1,2,4]-triazole-3-thiones complex: Design, sonochemical synthesis, and antimicrobial evaluation
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A series of new 1,2,4-triazole-3-thiones were synthesized by calm, benign, no risk, eco-friendly, and energy efficient sequential reaction methodology like grinding and ultrasonic (US). In addition, 1,2,4-triazoles were prepared under conventional method and comparative study was done. The synthesized 1,2,4-triazoles were complexed with Ni(II) to produce nanoparticles complexes (NPC's) with average particle size vary from 55 to 100 nm (using scanning electron microscope technique) with good yields via both US and conventional techniques. X-ray diffraction technique and spectra analysis techniques were used to confirm the square planer geometry of the synthesized NPC's. Antimicrobial activity of the prepared 1,2,4-triazoles and their nickel complexes were studied which evaluated a high activity with complexes instead their triazoles.
- El-Sayed, Amira A.,Farag, Paula S.,Hemdan, Magdy M.
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p. 3428 - 3441
(2020/09/11)
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- 4-aminocoumarin based aroylthioureas as potential jack bean urease inhibitors; synthesis, enzyme inhibitory kinetics and docking studies
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Background: Urease enzyme catalyzes the hydrolysis of urea into ammonia and CO2, excess ammonia causes global warming and crop reduction. Ureases are also responsible for certain human diseases such as stomach cancer, peptic ulceration, pyelone
- Abbas, Qamar,Ashraf, Zaman,Channar, Pervaiz A.,Fattah, Tanzeela A.,Hassan, Mubashir,Larik, Fayaz A.,Saeed, Aamer
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p. 229 - 243
(2020/03/06)
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- Synthesis of New N-Benzoyl-N'-Triazine Thiourea Derivatives and Their Antibacterial Activity
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Abstract: A series of new N-benzoyl-N'-triazine thiourea derivatives have been synthesized via the reaction of 4-amino-6-methyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one with benzoyl chloride derivatives and ammonium thiocyanate in acetone under reflux conditions. 4-Amino-6-methyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one was prepared from the reaction of two equivalents of hydrazine hydrate with carbon disulfide and sodium pyruvate. The chemical structure of thioureas was confirmed using FT-IR, 1H NMR, 13C NMR, and high-resolution mass spectrometry, and elemental analysis. The synthesized thioureas were assayed for their antibacterial activity against both gram-positive (Micrococcusluteus and Bacilluscereus) and gram-negative (Pseudomonasaeruginosa and Escherichiacoli) bacteria using the agar well diffusion method.
- Marzi,Pourshamsian,Hatamjafari,Shiroudi,Oliaey
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p. 391 - 397
(2019/10/28)
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- Synthesis of Novel Triazolyl Thiourea Derivatives and Their Antibacterial Activity
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4-Amino-5-methyl-2,4-dihydro-3H-1,2,4-triazole-3-thione was synthesized in three steps from carbon disulfide, hydrazine hydrate, and acetic acid. Its reaction with benzoyl isothiocyanates prepared from substituted benzoyl chlorides and ammonium thiocyanate afforded the corresponding N-benzoyl-N′-triazolyl-thioureas. The obtained compounds were screened for antibacterial activity against Staphylococcus aureus (ATCC 25923), Staphylococcus epidermidis (ATCC 12228), Enterococcus faecalis (ATCC 29212), Escherichia coli (ATCC 25922), and Pseudomonas aeruginosa (ATCC 27853). Their antibacterial activity against gram-positive bacteria was higher than against gram-negative bacteria, and derivatives containing electron-withdrawing groups were more active than those with electron-donating substituents.
- Kazeminejad,Pourshamsian,Hatamjafari,Shiroudi,Oliaey
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p. 1609 - 1615
(2019/12/28)
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- Synthesis and computational study of new meta- and para-substituted ferrocenyl thioureas as potent protein kinase inhibitors and cytotoxic agents
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The present study describes the synthesis, characterization, DNA binding and in vitro biological evaluation of ferrocene-enhanced thioureas. The new complexes (N1–N6) were prepared by reacting ferrocenyl anilines (A-B) with freshly prepared isothiocyanates in dry acetone. A crystallographic study of N3 revealed a supramolecular structure involving secondary non-covalent interactions (π?H and π?π). The nature and extent of the binding of these complexes with the salmon sperm DNA (SS-DNA) were examined by cyclic voltammetry and UV–Vis spectroscopy. The complexes have strong binding to DNA with binding constants ranging from 9.83 × 103 to 5.76 × 104 M?1. The shifts in the cathodic peak potentials with the addition of DNA in the electrochemical studies of the new complexes are attributed to electrostatic interactions. This observation is an indicator of the oxidizable behavior of the complexes in the presence of DNA. The theoretically calculated energies of the frontier molecular orbitals (EHOMO and ELUMO) and the Mulliken charge distributions for the optimized structures determined by the DFT/B3LYP method correlate well with the electrochemically determined redox potentials (correlation coefficient, 0.986). The computational measurements also led to a close agreement between the calculated and observed vibrational frequencies. The new complexes proved to be good candidates for protein kinase inhibition and cytotoxicity studies.
- Asghar, Faiza,Lal, Bhajan,Badshah, Amin,Butler, Ian S.,Nawaz Tahir, Muhammad
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- Solution-phase microwave assisted parallel synthesis, biological evaluation and in silico docking studies of 2-chlorobenzoyl thioureas derivatives
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An efficient and facile microwave-assisted solution phase parallel synthesis for a 38-member library of N-aroyl-N′-aryl thioureas was accomplished successfully. These analogues (1–38) were synthesized under identical set of conditions. It has been observe
- Khan, Muhammad Riaz,Zaib, Sumera,Rauf, Muhammad Khawar,Ebihara, Masahiro,Badshah, Amin,Zahid, Muhammad,Nadeem, Muhammad Arif,Iqbal, Jamshed
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p. 354 - 362
(2018/05/29)
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- Investigation of novel pesticides with insecticidal and antifungal activities: Design, synthesis and SAR studies of benzoylpyrimidinylurea derivatives
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In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by 1H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 μg mL?1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 μg mL?1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments.
- Chen, Peiqi,Song, Xiangmin,Fan, Yongmei,Kong, Weihao,Zhang, Hao,Sun, Ranfeng
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- Synthesis, carbonic anhydrase inhibitory activity and antioxidant activity of some 1,3-oxazine derivatives
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(Table presented.). A series of 1-(6-methyl-2-substituted phenyl-4-thioxo-4H-1,3-oxazin-5-yl)ethanones (3a-n) were synthesized by the reaction of benzoyl isothiocyanates with active methylene compound acetylacetone in the presence of triethyl amine in a one-pot process. The structures of the products were elucidated by elemental analyses, FT-IR, 1H NMR, 13C NMR, and mass spectroscopy. These new 1,3-oxazine derivatives were evaluated for their inhibitory activity against carbonic anhydrase II. Results for in vitro assay revealed that compound 3b having 4-methoxy phenyl moiety was the most potent inhibitor with IC50 value of 0.144 ± 0.008 μM. It exhibited higher enzyme inhibitory activity as compared to the standard acetazolamide (IC50 = 0.997 ± 0.061 μM). The compounds 3c, 3h, and 3n also displayed superior inhibitory activities compared to the rest of the synthesized oxazine derivatives. The radical scavenging activity of oxazine derivatives was also performed and it was found that compounds showed moderate antioxidant activity. Lipinski rule confirmed the therapeutic potential of the synthesized compounds. Molecular docking studies were also performed to further understand the binding affinity of these compounds with PDBID 1V9E which confirmed that the synthesized derivatives bind in the active binding site of the target protein. Based upon our results, it is proposed that compound 3b may serve as a lead structure to design more potent carbonic anhydrase inhibitors.
- Qamar, Rabia,Saeed, Aamer,Saeed, Maria,Ashraf, Zaman,Abbas, Qamar,Hassan, Mubashir,Albericio, Fernando
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p. 352 - 361
(2018/10/20)
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- Mononuclear copper(I) complexes with triphenylphosphine and N,N′-disubstituted thioureas: synthesis, characterization, and biological evaluation
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Twelve new complexes, of the general formula CuCl(TPP)2Tu1–12 (Tu = thiourea), were synthesized by the reaction of CuCl(TPP)3 (TPP = triphenylphosphine) and various N,N′-disubstituted thioureas. The structures of the synthesized complexes were characterized by different techniques such as Fourier transform infrared (FTIR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy (1H, 13C, 31P, and 19F), and the representative complexes (1, 2 and 12) were analyzed via single crystal X-ray diffraction. The single crystal X-ray analysis revealed that copper(I) is coordinated with chlorine, two TPP, and the thiourea ligands through the sulfur atom in a mononuclear distorted tetrahedral mode. The compounds were tested for antibacterial, antifungal, cytotoxicity, antileishmanial, and antioxidant activities. The results showed that the synthesized complexes are significantly more active than the free ligands and the commercial reference compounds. The high biological activities of the complexes versus free ligands can be attributed to the copper(I) chloride complexation with thiourea ligands. The synthesized complexes were also evaluated, both experimentally and theoretically, for DNA binding studies. The UV-visible spectroscopic and molecular docking studies demonstrated that the complexes are conjugating with DNA through a groove binding mode.
- Khan, Syed Ishtiaq,Ali Khan, Inayat,Badshah, Amin,Perveen Malik, Fouzia,Tabassum, Saira,Ullah, Ikram,Zargarian, Davit,Khawar Rauf, Muhammad
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p. 4086 - 4108
(2018/12/04)
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- Phosphine-free direct conversion of carboxylic acids into acyl isothiocyanates using various electrophilic halogenation reagents
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In this study, the efficiency of some electrophilic halogen reagents including 2,4,6-trichloro-1,3,5-triazine, 2,4,4,6-tetrabromo-2,5-cyclohexadienone, 2-chloro-1-methylpyridinium iodide, N-bromosuccinimide, trichloroisocyanuric acid, and 1,3-dibromo-5,5-
- Khaje-Kolaki, Aslan,Mokhtari, Babak
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p. 805 - 808
(2018/09/26)
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- Biologically active: Halo -substituted ferrocenyl thioureas: Synthesis, spectroscopic characterization, and DFT calculations
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In our search for new therapeutic agents, ferrocene-based thioureas (M1-M9) were successively synthesized and characterized by various analytical techniques like FT-IR, Raman, CHNS, AAS, and multinuclear (1H and 13C) NMR. The interac
- Asghar, Faiza,Rana, Sadaf,Fatima, Saira,Badshah, Amin,Lal, Bhajan,Butler, Ian S.
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p. 7154 - 7165
(2018/05/04)
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- Synthesis of sulfadiazinyl acyl/aryl thiourea derivatives as calf intestinal alkaline phosphatase inhibitors, pharmacokinetic properties, lead optimization, Lineweaver-Burk plot evaluation and binding analysis
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To seek the new medicinal potential of sulfadiazine drug, the free amino group of sulfadiazine was exploited to obtain acyl/aryl thioureas using simple and straightforward protocol. Acyl/aryl thioureas are well recognized bioactive pharmacophore containin
- Sajid-ur-Rehman,Saeed, Aamer,Saddique, Gufran,Ali Channar, Pervaiz,Ali Larik, Fayaz,Abbas, Qamar,Hassan, Mubashir,Raza, Hussain,Fattah, Tanzeela Abdul,Seo, Sung-Yum
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p. 3707 - 3715
(2018/06/19)
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- Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one derivatives containing thiourea and acylthiourea against Meloidogyne incognita
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Two series of novel 1,2,3-benzotriazin-4-one derivatives containing thiourea and acylthiourea were designed and synthesized. The bioassay results showed that most of the test compounds showed good nematicidal activity against M. incognita at the concentration of 10.0?mg?L?1 in vivo. The compounds A13, A17 and B3 showed excellent nematicidal activity on the second stage juveniles of the root-knot nematode with the inhibition rate of 51.3%, 58.3% and 51.3% at the concentration of 1.0?mg?L?1 respectively. It suggested that the structure of 1,2,3-benzotriazin-4-one derivatives containing thiourea and acylthiourea could be optimized further.
- Chang, Yaning,Zhang, Jingwei,Chen, Xiulei,Li, Zhong,Xu, Xiaoyong
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p. 2641 - 2644
(2017/05/10)
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- Synthesis of novel derivatives of chromenone bearing an N-carbamothioyl moiety as soybean 15-LOX inhibitors
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Novel derivatives of chromenone bearing an N-carbamothioyl moiety were synthesized and evaluated for their soybean 15-LOX inhibitory activity. Synthesis of the target compounds was started from 7-hydroxy-2H-chromen-2-one. It was reacted with 1-fluoro-2(4)
- Kaviani, Robabeh,Saeedi, Mina,Mahdavi, Mohammad,Nadri, Hamid,Moradi, Alireza,Shafiee, Abbas,Akbarzadeh, Tahmineh
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p. 335 - 344
(2017/07/04)
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- Synthesis and antitumor activity of novel N-benzoyl-N'-substituted pyrimidinyl (thio)semicarbazide derivatives
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A series of substituted pyrimidinyl (thio)semicarbazide derivatives were designed and synthesized. The antitumor results showed that the activity of thiosemicarbazide compounds (series II) was generally higher than that of the corresponding semicarbazide derivatives (series I). Among them, IIk displayed higher cytotoxicity against HL-60, BGC-823 and Bel-7402 than that of adriamycin and exhibited broad in vitro cytotoxicity against 13 human tumor cell lines. Meanwhile, the cytotoxic selectivity and anti-multidrug resistance were evaluated, and IIk exhibited selective cytotoxicity against cancer cells in comparison to human normal cells and had significant anti-multidrug resistance capability. The bioassay results showed that IIk showed great promise as a potent lead compound for further antitumor discovery.
- Song, Gaopeng,Li, Jianzuo,Tian, Hao,Li, Yasheng,Hu, Dekun,Li, Ying,Cui, Zining
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p. 329 - 334
(2016/04/04)
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- Synthesis, characterization, crystal structures, analgesic and antioxidant activities of thiourea derivatives
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1-(2-chlorobenzoyl)-3-(2,3-dimethyl-5-oxo-1-phenyl-2,5-dihydro-1H-pyrazol-4-yl)thiourea (Cl2AAP) and 1-(2-chlorobenzoyl)-3-(pyridine-2-yl)thiourea (Cl2AP) were synthesized and characterized by spectroscopic methods (FT-IR, 1H NMR) and single crystal X-ray diffraction. Both compounds crystallized in monoclinic system and solved in P21/n, Z = 4 and P21/c, Z = 12 space groups respectively. Pharmacological screenings of the synthesized compounds have shown comparable analgesic activity to that of the standard diclofenac sodium at 30 mg/kg body weight dose. The DPPH and ABTS free radical scavenging activity of Cl2AAP are more significant than Cl2AP as compared to standard (IC50= 10, 60; 45, 75; and 10 μg/ml for standard Ascorbic acid respectively).
- Shoaib, Mohammad,Shafiullah,Ayaz, Muhammad,Tahir, Muhammad Nawaz,Shah, Syed Wadood Ali
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p. 479 - 486
(2016/08/28)
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- Biological evaluation of halogenated thioureas as cholinesterases inhibitors against alzheimer's disease & molecular modeling studies
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Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition is thought to be an encouraging approach towards the therapy of Alzheimer's disease (AD). The current paper targets to give a concise information of mono and dihalo- substituted thioureas similarity with anti-AD potential. The present results represent evaluation of cholinesterase inhibitory potential for halogenated thioureas derivatives. Compound 1t was constituted to be highly potent inhibitor with Ki value 0.12 ± 0.05 μM against AChE, while 1b was most the active inhibitor for BChE with Ki value of 0.03 ± 0.001 μM. Molecular docking simulations were performed using the homology models of both cholinesterases in order to explore the plausible binding modes of synthesized compounds.
- Iqbal, Jamshed,Zaib, Sumera,Saeed, Aamer,Muddassar, Muhammad
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p. 488 - 494
(2015/06/22)
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- Structure-Activity Relationships and Anti-inflammatory Activities of N-Carbamothioylformamide Analogues as MIF Tautomerase Inhibitors
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Macrophage migration inhibitory factor (MIF), a proinflammatory cytokine, is an attractive therapeutic target for the treatment of inflammatory diseases. In our previous study, 3-[(biphenyl-4-ylcarbonyl)carbamothioyl]amino benzoic acid (compound 1) was discovered as a potent inhibitor of MIF by docking-based virtual screening and bioassays. Here, a series of analogues of compound 1 derived from similarity search and chemical synthesis were evaluated for their MIF tautomerase activities, and their structure-activity relationships were then analyzed. The most potent inhibitor (compound 5) with an IC50 of 370 nM strongly suppressed lipopolysaccharide (LPS)-induced production of TNF-α and IL-6 in a dose-dependent manner and significantly enhanced the survival rate of mice with LPS-induced endotoxic shock from 0 to 35% at 0.5 mg/kg and to 45% at 1 mg/kg, highlighting the therapeutic potential of the MIF tautomerase inhibition in inflammatory diseases.
- Zhang, Yu,Xu, Lei,Zhang, Zhiqiang,Zhang, Zhiyu,Zheng, Longtai,Li, Dan,Li, Youyong,Liu, Feng,Yu, Kunqian,Hou, Tingjun,Zhen, Xuechu
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p. 1994 - 2004
(2015/10/06)
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- Design, syntheses and evaluation of benzoylthioureas as urease inhibitors of agricultural interest
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Urea is one of the most used nitrogen fertilizers worldwide. However, occurrence of urea hydrolysis to ammonia and carbon dioxide on soil surface, catalyzed by soil ureases, considerably reduces nitrogen availability to crops. In this study, we describe the design, synthesis and screening of sixty five benzoylthioureas (BTUs) for their ability to inhibit purified jack bean and soil ureases. BTUs were readily obtained in one pot, two steps synthesis with no need of cumbersome procedures for product purification. In vitro assays revealed BTUs 11, 12, 14, 19-22 and 37 as the most active jack bean urease inhibitors. Such BTUs were found to be able to bind to both catalytic and allosteric sites of urease, acting therefore as mixed-type inhibitors. Out of 28 compounds that effectively inhibited soil ureases activity, BTUs 3, 6, 10, 12, 16, 19 and 22 were determined to be more potent than the reference inhibitor N-(butyl) thiophosphoric triamide (NBPT; 40%). The other 22 BTUs were as potent as NBPT on soil ureases. The temperature-tolerance of BTUs, along with their ability to inhibit soil ureases, makes of this class of compounds potential additive for urea-based fertilizers.
- Brito, Tiago O.,Souza, Aline X.,Mota, Yane C. C.,Morais, Vinicius S. S.,De Souza, Leandro T.,De Fátima, ?ngelo,Macedo, Fernando,Modolo, Luzia V.
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p. 44507 - 44515
(2015/06/02)
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- Straightforward Approach Toward Dihydrothiazoles via Intramolecular Bromocyclization
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An intramolecular bromonium ion-assisted cyclization with sulfur as an internal nucleophile is described. Starting from benzoyl chlorides, this method provides an easy procedure for the synthesis of dihydrothiazole derivatives in moderate to good yields.
- Sadat-Ebrahimi, Seyed Esmail,Ganjizadeh Zarj, Marzieh,Moghimi, Setareh,Yahya-Meymandi, Azadeh,Mahdavi, Mohammad,Arab, Saman,Shafiee, Abbas,Foroumadi, Alireza
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p. 2142 - 2147
(2015/09/01)
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- Synthesis, structural characterization, DNA binding and antioxidant potency of new ferrocene incorporated acyl ureas
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In this article, we have reported the synthesis of three new ferrocene incorporated ureas namely; 1-(4-Chlorobenzoyl)-3-(4-ferrocenylphenyl)urea (P4Cl), 1-(3-Chlorobenzoyl)-3-(4-ferrocenyl phenyl)urea (P3Cl) and 1-(2-Chlorobenzoyl)-3-(4-ferrocenylphenyl)urea (P2Cl). All new compounds were unambiguously characterized by common analytical techniques (NMR, FT-IR, AAS, CHNS and molecular docking). Furthermore, single crystal XRD analysis was done for 1-(3-Chlorobenzoyl)-3-(4-ferrocenylphenyl)urea. DNA binding is a pre-requisite for a compound to be used as an antitumor agent. The DNA binding study was done by cyclic voltammetry, UV-vis spectroscopy and viscometry. The drug-DNA binding constant was found to vary in the sequence: KP2Cl (6.056 × 104 M-1) > KP4Cl (5.713 × 104 M-1) > KP3Cl (4.631 × 104 M-1). Diffusion coefficient of the drug-DNA adduct for all the compounds is lower than the free drug, indicating that drug-DNA adduct is of higher molecular weight and slow diffusing as compared to the free drug. Small binding site size of 0.440 (P3Cl), 0.585 (P4Cl) and 0.673 (P2Cl) base pairs is consistent with electrostatic interaction. All the compounds exhibited good antioxidant activities with IC50 values of 82, 136 and 54 μM for P4Cl, P3Cl and P2Cl respectively, against DPPH.
- Asghar, Faiza,Badshah, Amin,Hussain, Raja Azadar,Sohail, Manzar,Akbar, Kamran,Butler, Ian Sydney
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p. 131 - 139
(2015/09/07)
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- Direct and facile synthesis of acyl isothiocyanates from carboxylic acids using trichloroisocyanuric acid/triphenylphosphine system
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A mild, efficient, and practical method for one-step synthesis of alkanoyl and aroyl isothiocyanates from carboxylic acids using a safe and inexpensive mixed reagent, trichloroisocyanuric acid/triphenyl-phosphine is described at room temperature. Availability of the reagents and easy workup of the reaction make this method attractive for organic chemists.
- Entezari, Najmeh,Akhlaghinia, Batool,Rouhi-Saadabad, Hamed
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p. 201 - 206
(2015/02/05)
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- Synthesis, biological evaluation and docking study of 3-aroyl-1-(4- sulfamoylphenyl)thiourea derivatives as 15-lipoxygenase inhibitors
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A series of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives containing sulfonamide moiety were designed and synthesized as 15-lipoxygenase (15-LOX) inhibitors. Most synthesized compounds showed potent activity against soybean 15-LOX with IC50
- Mahdavi, Mohammad,Shirazi, Maryam Shahzad,Taherkhani, Raana,Saeedi, Mina,Alipour, Eskandar,Moghadam, Farshad Homayouni,Moradi, Alireza,Nadri, Hamid,Emami, Saeed,Firoozpour, Loghman,Shafiee, Abbas,Foroumadi, Alireza
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p. 308 - 313
(2014/06/24)
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- New aminobenzenesulfonamide-thiourea conjugates: Synthesis and carbonic anhydrase inhibition and docking studies
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A variety of 1-substituted-3-(3-aminosulfonylphenyl)thioureas (3a-k) and two new 1-aroyl-3-(4-aminosulfonylphenyl)thiourea derivatives (5a and 5b) were synthesized by reaction of 3-aminobenzenesulfonamide and 4- aminobenzenesulfonamide respectively with f
- Zaib, Sumera,Saeed, Aamer,Stolte, Karin,Fl?rke, Ulrich,Shahid, Mohammad,Iqbal, Jamshed
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p. 140 - 150
(2014/04/17)
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- Antituberculosis and antifungal activities of synthesized, benzoylthiourea derivatives
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A series of benzoylthiourea derivatives have been synthesized from benzoyl isothiocyanate and phenyleneamine in CH2Cl2 medium under solid-liquid phase transfer catalysis conditions. Structures of these compounds have been characterized by elemental analyses as well as IR and 1H NMR spectroscopy. All the compounds were tested for their antibacterial and antifungal activities, the results indicated that most of the compounds have antibacterial and antifungal activities close to the standard drugs, especially they were found to have remarkable antituberculosis and antifungal activities.
- Zhao, Meng-Meng,Dong, Xiu-Yan,Li, Gang,Yang, Yu-Hua,Zhang, Yu-Jie,Yang, Xiao-Qin
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p. 7548 - 7550
(2013/08/23)
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- Synthesis, characterization and antibacterial activity of new 1,2- and 1,4-bis(n'-substituted thioureido)benzene derivatives
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Synthesis of two series of 1,2- and 1,4-bis(thioureido)benzene derivatives was accomplished by the treatment of corresponding alkanoyl/aroyl chlorides with potassium thiocyanate in dry acetone to afford the respective isothiocyanates as intermediates. The
- Saeed, Aamer,Abbas, Naeem,Ashraf, Zaman,Bolte, Michael
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p. 273 - 278
(2013/12/04)
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- Hybrid molecules of carvacrol and benzoyl urea/thiourea with potential applications in agriculture and medicine
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Benzoyl phenyl urea, a class of insect growth regulator's acts by inhibiting chitin synthesis. Carvacrol, a naturally occurring monoterpenoid is an effective antifungal agent. We have structurally modified carvacrol (2-methyl-5-[1-methylethyl] phenol) by introducing benzoylphenyl urea linkage. Two series of benzoylcarvacryl thiourea (BCTU, 4a-f) and benzoylcarvacryl urea (BCU, 5a-f) derivatives were prepared and characterized by elemental analysis, IR, 1H and 13C NMR and Mass spectroscopy. Derivatives 4b, 4d, 4e, 4f and 5d, 5f showed comparable insecticidal activity with the standard BPU lufenuron against Dysdercus koenigii. BCTU derivatives 4c, 4e and BCU 5c showed good antifungal activity against phytopathogenic fungi viz. Magnaporthe grisae, Fusarium oxysporum, Dreschlera oryzae; food spoilage yeasts viz. Debaromyces hansenii, Pichia membranifaciens; and human pathogens viz. Candida albicans and Cryptococcus neoformans. Compounds 5d, 5e and 5f showed potent activity against human pathogens. Moderate and selective activity was observed for other compounds. All the synthesized compounds were non-haemolytic. These compounds have potential application in agriculture and medicine.
- Pete, Umesh D.,Zade, Chetan M.,Bhosale, Jitendra D.,Tupe, Santosh G.,Chaudhary, Preeti M.,Dikundwar, Amol G.,Bendre, Ratnamala S.
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supporting information; experimental part
p. 5550 - 5554
(2012/09/22)
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- β-Enaminonitriles in heterocyclic synthesis: Synthesis of new 1,4-dihydropyridine, tetrahydropyridine, nicotinonitrile and aminopyrazole derivatives
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A series of new pyridine, dihydropyridine, tetrahydropyridine, nicotinonitrile and pyrazole derivatives with expected biological activity were prepared through the reactions of 3-aminopent-2-enenitrile 1 with some electrophilic reagents, nucleophilic reagents, and aryl diazonium salts. The newly synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR and mass spectral studies.
- Ramiz, Mahmoud M. M.,Abdel Hafiz, Ibrahim S.,Elian, Mohamed A.
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experimental part
p. 758 - 767
(2012/08/29)
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- SAR analysis of a series of acylthiourea derivatives possessing broad-spectrum antiviral activity
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A series of acylthiourea derivatives were designed, synthesized, and evaluated for broad-spectrum antiviral activity with selected viruses from Poxviridae (vaccinia virus) and two different genera of the family Bunyaviridae (Rift Valley fever and La Cross
- Burgeson, James R.,Moore, Amy L.,Boutilier, Jordan K.,Cerruti, Natasha R.,Gharaibeh, Dima N.,Lovejoy, Candace E.,Amberg, Sean M.,Hruby, Dennis E.,Tyavanagimatt, Shanthakumar R.,Allen III, Robert D.,Dai, Dongcheng
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scheme or table
p. 4263 - 4272
(2012/07/17)
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- Novel and efficient cyclization procedure for the synthesis of 2,5-disubstituted-1,3,4-thiadiazoles without using any ring-closing reagents
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A novel method for the synthesis of 2,5-disubstituted-1,3,4-thiadiazoles via direct ring closure of 1,6-disubstituted-2,5-dithioureas in dimethylformanide without using any ring-closing reagents has been accidentally discovered. Repeated and extended experiments confirmed that this is a very simple and efficient way to synthesize these kinds of fine chemicals. A series of novel 2,5-disubstituted-1,3,4-thiadiazoles have been synthesized via this method in good yields.
- Lin, Qi,Zhang, You-Ming,Li, Man-Lin,Wei, Tai-Bao
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experimental part
p. 3251 - 3260
(2012/09/10)
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- Activated anilide in heterocyclic synthesis: Synthesis of new dihydropyridines, dihydropyridazines and thiourea derivatives
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A series of new dihydropyridines, butanamide, dihydropyridazines and thiourea derivatives have been prepared through the reactions of 3-aminopyridine (1) and N-(pyridin-3-yl)-3-(pyridin-3-ylimino)butanamide 3 with some electrophilic reagents, aryl diazonium salts and isothiocyanates. Elementary analysis, MS, IR, and 1H NMR spectra confirmed the identity of the products. Copyright
- Hafiz, Ibrahim S.A.,Ramiz, Mahmoud M.M.,Sarhan, Ahmed A.M.
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experimental part
p. 1154 - 1162
(2012/03/26)
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- New substituted thiazol-2-ylidene-benzamides and their reaction with 1-Aza-2-azoniaallene salts. Synthesis and anti-HIV activity
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Aseries of N-(3-(substituted-aikyl- or halophenyl)-4-methylthiazol-2(3H)- ylidene)-substituted alkyl- or halo-benzamides 21-40 were prepared by base-catalyzed cyclization of the corresponding 1-(substituted-alkyl- or halo-benzoyl)-3-(substituted-halophenyl)thioureas 1-20. Substituted pyrazolo[4,3-d]thiazol-5(6aH)-ylidene)benzamides 45a-d were synthesized by cycloaddition of compound 45 with the reactive cumulene intermediates 42a -d. All compounds were evaluated for their antiviral activity against the replication of HIV-1 and HIV-2 in MT-4. Compounds 35 and 39 showed an IC 50 of 2.02 μgmL-1 and 0.40 μgmL-1 against the HIV-2 strain ROD with CC50 of ≥ 104.00 μgmL-1 and > 125.00 μgmL-1, respectively, resulting in a selectivity index of ≥ 52 and > 313. Based on the chemical structure of compounds 35 and 39, these molecules can be proposed to act as NNRTIs. However, it is exceptional to observe an antiretroviral activity that is limited to HIV-2.
- Saeed, Aamer,Al-Masoudi, Najim A.,Ahmed, Amjed A.,Pannecouque, Christophe
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body text
p. 512 - 520
(2011/07/08)
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- A novel series of 2,5-disubstituted 1,3,4-thiadiazoles as potential anticonvulsant agent
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In pursuit for better antiepileptic drug and the importance of semicarbazones and 2,5-disubstituted 1,3,4-thiadiazoles as anticonvulsant pharmacophore, a series of novel N-({5-[(6-methyl-1-benzofuran-3-yl)methyl]-1,3,4-thiadiazol-2-yl}carbamothioyl)-2/3/4-substitutedbenzamide were designed, synthesized and evaluated for their anticonvulsant activity. The findings of the present studies confirmed that the pharmacophore model with four binding sites is crucial for anticonvulsant activity. Structure-activity relationships among synthesized compounds were also established.
- Rajak, Harish,Behera, Chinmay K.,Pawar, Rajesh S.,Singour, Pradeep K.,Kharya, Murli Dhar
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p. 1149 - 1152
(2011/10/08)
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- Synthesis, characterization and antimicrobial activity of some new 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas
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Synthesis of a variety of new 1-(isomeric fluorobenzoyl)-3-(isomeric fluorophenyl)thioureas (1a-t) was accomplished in two steps. The synthetic route involves the reaction of equimolar quantities of isomeric fluorobenzoyl chlorides with potassium thiocyanate in anhydrous acetone to afford the corresponding isothiocyantes in situ, followed by treatment with equimolar quantities of isomeric fluoroanilines. All of the synthesized compounds (1a-t) were screened for their in vitro antibacterial activity using Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aureginosa). The minimum inhibitory concentration (MIC) was also determined for the most active compounds. In vitro antifungal activity was also determined against the five fungal species (Rhizopus oryzae, Aspergillus tereus, Fusarium oxysporum, Aspergillus niger, Aspergillus fumigatus). In general, the antifungal activity of compounds was better than their antibacterial activity.
- Saeed, Aamer,Shaheen, Uzma,Hameed,Naqvi, S.Z. Haider
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experimental part
p. 1028 - 1034
(2010/04/28)
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- N-{[(6-Substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: Synthesis and pharmacological evaluation
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A series of 1,3-benzothiazol-2-yl benzamides (11-30) were prepared in satisfactory yield and evaluated for their anticonvulsant, neurotoxicity, CNS depressant study and other toxicity studies. All the synthesized compounds were in good agreement with elemental and spectral data. Majority of the compounds were active in MES and scPTZ screen and showed the decrease in the immobility time. None of the compounds had shown neurotoxicity or liver toxicity.
- Rana, Arpana,Siddiqui, Nadeem,Khan, Suroor A.,Ehtaishamul Haque, Syed,Bhat, Mashooq A.
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p. 1114 - 1122
(2008/09/21)
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- Synthesis and crystal structure of some novel 2-aroylimino-3-aryl-4-phenyl- 1,3-thiazolines
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An efficient synthesis of some novel 2-aroylimino-3-aryl-4-phenyl-1,3- thiazolines was carried out by base-catalyzed cyclization of 1-aroyl-3-arylthioureas with acetophenone in the presence of bromine. The structures were confirmed by spectroscopic data,
- Saeed, Aamer,Zaman, Sabah,Bolte, Michael
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p. 2185 - 2199
(2008/09/21)
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