- In silico and antithrombotic studies of 1,3,4-oxadiazoles derived from benzimidazole
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In the present study, a series of 1,3,4-oxadiazole derivatives (4a-4k) derived from benzimidazole were docked onto factor Xa (PDB: 1NFY) protein using SYBYLX 2.1. and also evaluated for in vitro clot lysis for thrombolytic activity. The synthesized molecules were also screened for in silico ADME studies. The molecular docking studies highlighted that the molecules showed high affinity towards 1NFY with higher docking score and the in silico ADME results were promising and indicated that the molecules holds great potential as a drug candidate. The thrombolytic evaluation was performed for decrease in solid clot weight by the clot lysis study at a concentration of 6.25, 12.5 and 25 μM strengths, respectively. The results of in vitro clot lysis for thrombolytic evaluation revealed that the tested compounds 4a-4k exhibited significant clot lysis with respect to negative control phosphate buffered saline and in comparison to the reference drug streptokinase (30,000 IU). Among all the tested compounds, compound 4j, 4d and 4g exhibited potent thrombolytic activity with EC50 value of 16.2, 18.1 and 23.7 μM, respectively. The thrombolytic efficacy investigation highlights that the synthesized compound 4j could be considered for further clinical studies to ascertain its possible hit as thrombolytic agents.
- Vishwanathan,Gurupadayya,Venkata Sairam
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Read Online
- Synthesis and biological research of novel azaacridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors
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DNA and DNA-related enzymes are one of the most effective and common used intracellular anticancer targets in clinic and laboratory studies, however, most of DNA-targeting drugs suffered from toxic side effects. Development of new molecules with good antitumor activity and low side effects is important. Based on computer aided design and our previous studies, a series of novel azaacridine derivatives were synthesized as DNA and topoisomerases binding agents, among which compound 9 displayed the best antiproliferative activity with an IC50 value of 0.57?μM against U937 cells, which was slightly better than m-AMSA. In addition, compound 9 displayed low cytotoxicity against human normal liver cells (QSG-7701), the IC50 of which was more than 3 times lower than m-AMSA. Later study indicated that all the compounds displayed topoisomerases II inhibition activity at 50?μM. The representative compound 9 could bind with DNA and induce U937 apoptosis through the exogenous pathway.
- Li, Dan,Yuan, Zigao,Chen, Shaopeng,Zhang, Cunlong,Song, Lu,Gao, Chunmei,Chen, Yuzong,Tan, Chunyan,Jiang, Yuyang
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Read Online
- The design and synthesis of potent benzimidazole derivatives via scaffold hybridization and evaluating their antiproliferative and proapoptotic activity against breast and lung cancer cell lines
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One of the current approaches used in drug discovery and development is the synthesis of novel small compounds from existing structural motifs via molecular hybridization. In the current study, a new series of benzimidazo[1,5-a]imidazole, benzimidazo[1,2-c]thiazole, benzimidazotriazine, and benzimidazo[1,2-c]quinazoline scaffolds was synthesized via C-H cycloamination, using a metal-free synthetic pathway, as potent antiproliferative antiangiogenic molecules against breast (MCF-7) and lung (A549) cancer cell lines. The expansion of the benzimidazole scaffold with heterocyclic rings resulted in a tridentate cyclic system that occupied the ATP-binding site and neighboring hydrophobic pocket, eliciting promising affinity and selectivity toward VEGFR2 through extra H-bonding and completely occupying the entrance region. Molecular docking studies demonstrated that most of the designed compounds bind VEGFR-2 adopting a DFG-in conformation, where the benzimidazole scaffold occupied the hinge region, the central aromatic ring occupied hydrophobic region I adjacent to the hinge region, and the hydrogen bond donor/acceptor bound to the hydrogen-bond-rich region. In comparison to lenvatinib, which had a docking score of-12.47 kJ mol-1 and a Glide E-model value of-132.68 kcal mol-1, compound 17 had a decent docking score of-8.95 kJ mol-1 and a Glide E-model value of-92.17 kcal mol-1. The designed molecules exhibited promising in situ cytotoxic activities, with IC50 values ranging from 9.2 to 42.3 μM against MCF-7 and A549, comparable to 5-fluorouracil (which has IC50 values of 10.32 and 5.8 μM against MCF-7 and A549, respectively); they also showed selective in vitro inhibitory activity against VEGFR2 when compared with other designed kinases, with compound 17 showing an IC50 value (23 nM) as good as that of sorafenib (30 nM). Flow cytometry and cell cycle assays revealed that apoptotic cell death induction occurred in the A549 cell line through the activation of certain caspases and the tumor suppressor P53 and through repressing the generation of BAX and PUMA. Furthermore, the proposed compounds exhibited physicochemical and pharmacokinetics properties within the acceptable range for human usage, as anticipated by an in silico ADME study, making them lead molecules for developing new forms of medication.
- Elgawish, Mohamed Saleh,Ghareb, Nagat,Nafie, Mohamed S.,Yamada, Koji,Yassen, Asmaa S. A.
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p. 4239 - 4256
(2022/03/14)
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- Cu(II) complex-decorated hybrid nanomaterial: a retrievable catalyst for green synthesis of 2,3-dihydroquinazolin-4(1H)-ones
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The significant stability of magnetic core and ? OH functional groups on the surface of silica-coated cobalt ferrite (CoFe2O4@SiO2) nanoparticles make it a good candidate for functionalization and catalytic application. In
- Bodaghifard, Mohammad Ali,Safari, Somayeh
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p. 1613 - 1627
(2021/04/26)
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- Synthesis and biological activity of squaramido-tethered bisbenzimidazoles as synthetic anion transporters
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A series of squaramido-tethered bisbenzimidazoles were synthesized from the reaction of diethyl squarate with substituted 2-aminomethylbenzimidazoles. These conjugates exhibit moderate binding affinity toward chloride anions. They are able to facilitate the transmembrane transport of chloride anions most probably via an anion exchange process, and tend to be more active at acidic pH than at physiological pH. The viability of these conjugates toward four selected solid tumor cell lines was evaluated using an MTT assay and the results suggest that some of these conjugates exhibit moderate cytotoxicity probably in an apoptotic fashion.
- Wang, Zhong-Kun,Hong, Xiao-Qiao,Hu, Jinhui,Xing, Yuan-Yuan,Chen, Wen-Hua
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p. 3972 - 3980
(2021/02/02)
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- Impact of N-Alkylamino Substituents on Serotonin Receptor (5-HTR) Affinity and Phosphodiesterase 10A (PDE10A) Inhibition of Isoindole-1,3-dione Derivatives
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In this study, a series of compounds derived from 4-methoxy-1H-isoindole-1,3(2H)-dione, potential ligands of phosphodiesterase 10A and serotonin receptors, were investigated as potential antipsychotics. A library of 4-methoxy-1H-isoindole-1,3(2H)-dione derivatives with various amine moieties was synthesized and examined for their phosphodiesterase 10A (PDE10A)-inhibiting properties and their 5-HT1A and 5-HT7 receptor affinities. Based on in vitro studies, the most potent compound, 18 (2-[4-(1H-benzimidazol-2-yl)butyl]-4-methoxy-1H-isoindole-1,3(2H)-dione), was selected and its safety in vitro was evaluated. In order to explain the binding mode of compound 18 in the active site of the PDE10A enzyme and describe the molecular interactions responsible for its inhibition, computer-aided docking studies were performed. The potential antipsychotic properties of compound 18 in a behavioral model of schizophrenia were also investigated.
- Czopek, Anna,Partyka, Anna,Bucki, Adam,Paw?owski, Maciej,Ko?aczkowski, Marcin,Siwek, Agata,G?uch-Lutwin, Monika,Koczurkiewicz, Paulina,P?kala, El?bieta,Jaromin, Anna,Tyliszczak, Bo?ena,Weso?owska, Anna,Zagórska, Agnieszka
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- Dibenzimidazole conjugates with pH dependent anion trans-membrane transport activity Synthesis method and synthesis method thereof (by machine translation)
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13-bis-benzimidazole conjugate is synthesized by the method, the chloride ion transport activity of each conjugate under the acidic pH condition is higher than the activity at physiological pH, and the synthesized conjugate also shows moderate intensity toxicity on selected solid tumor cells. (by machine translation)
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Paragraph 0072-0080
(2021/01/04)
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- Cooperative Mn(i)-complex catalyzed transfer hydrogenation of ketones and imines
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The synthesis and reactivity of Mn(i) complexes bearing bifunctional ligands comprising both the amine N-H and benzimidazole fragments are reported. Among the various ligands, the N-((1H-benzimidazol-2-yl)methyl)aniline ligand containing Mn(i) complex presented higher reactivity in the transfer hydrogenation (TH) of ketones in 2-propanol. Experimentally, it was established that both the benzimidazole and amine N-H proton played a vital role in the enhancement of the catalytic activity. Utilizing this system a wide range of aldehydes and ketones were reduced efficiently. Notably, the TH of several imines, as well as chemoselective reduction of unsaturated ketones, was achieved in the presence of this catalyst. DFT calculations were carried out to understand the plausible reaction mechanism which disclosed that the transfer hydrogenation reaction followed a concerted outer-sphere mechanism.
- Ganguli, Kasturi,Shee, Sujan,Panja, Dibyajyoti,Kundu, Sabuj
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p. 7358 - 7366
(2019/06/06)
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- Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer
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Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.
- Monastyrskyi, Andrii,Nilchan, Napon,Quereda, Victor,Noguchi, Yoshihiko,Ruiz, Claudia,Grant, Wayne,Cameron, Michael,Duckett, Derek,Roush, William
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p. 590 - 602
(2018/01/01)
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- α-Amino Acid Derived Benzimidazole-Linked Rhodamines: A Case of Substitution Effect at the Amino Acid Site toward Spiro Ring Opening for Selective Sensing of Al3+ Ions
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α-Amino acid derived benzimidazole-linked rhodamines have been synthesized, and their metal ion sensing properties have been evaluated. Experimentally, l-valine- and l-phenylglycine-derived benzimidazole-based rhodamines 1 and 2 selectively recognize Al3+ ion in aqueous CH3CN (CH3CN/H2O 4/1 v/v, 10 mM tris HCl buffer, pH 7.0) over the other cations by exhibiting color and "turn-on" emission changes. In contrast, glycine-derived benzimidazole 3 remains silent in the recognition event and emphasizes the role of α-substitution of amino acid undertaken in the design. The fact has been addressed on the basis of the single-crystal X-ray structures and theoretical calculations. Moreover, pink 1·Al3+ and 2·Al3+ ensembles selectively sensed F- ions over other halides through a discharge of color. Importantly, compounds 1 and 2 are cell permeable and have been used as imaging reagents for the detection of Al3+ uptake in human lung carcinoma cell line A549.
- Majumdar, Anupam,Mondal, Subhendu,Daniliuc, Constantin G.,Sahu, Debashis,Ganguly, Bishwajit,Ghosh, Sourav,Ghosh, Utpal,Ghosh, Kumaresh
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p. 8889 - 8899
(2017/08/14)
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- Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors
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Cancer metabolism and epigenetics are among the most intensely pursued research areas in anticancer drug discovery. Here we report the first small molecules that simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and histone deacetylase (HDAC), two important targets of cancer metabolism and epigenetics, respectively. Through iterative structure-based drug design, chemical synthesis, and biological assays, a highly potent dual NAMPT and HDAC inhibitor was successfully identified. Compound 35 possessed excellent and balanced activities against both NAMPT (IC50 = 31 nM) and HDAC1 (IC50 = 55 nM). It could effectively induce cell apoptosis and autophagy and ultimately led to cell death. Importantly, compound 35 showed excellent in vivo antitumor efficacy in the HCT116 xenograft model. This proof-of-concept study demonstrates the feasibility of discovering an inhibitor targeting cancer metabolism and epigenetics and provides an efficient strategy for multitarget antitumor drug discovery.
- Dong, Guoqiang,Chen, Wei,Wang, Xia,Yang, Xinglin,Xu, Tianying,Wang, Pei,Zhang, Wannian,Rao, Yu,Miao, Chaoyu,Sheng, Chunquan
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p. 7965 - 7983
(2017/10/18)
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- Facile synthesis, characterization and antimicrobial activity of 2-alkanamino Benzimidazole derivatives
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Benzimidazole derivatives are known to represent a class of medicinally important compounds which are extensively used in drug design and catalysis. A series of 2-substituted benzimidazole derivatives 10a-i was herein synthesized from the reaction of o-phenylenediamine with some amino acids using ameliorable pathway. The chemical structures of the synthesized compounds were confirmed by IR, UV, 1H-NMR, 13C-NMR, Mass spectral and analytical data. The compounds were investigated for their antimicrobial activity alongside gentamicin clinical standard. The results showed that this skeletal framework exhibited marked potency as antimicrobial agents. The most active compound was 1H-benzo[d]imidazol-2-yl)methanamine, 10a.
- Ajani, Olayinka O.,Aderohunmu, Damilola V.,Olorunshola, Shade J.,Ikpo, Chinwe O.,Olanrewaju, Ifedolapo O.
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p. 109 - 120
(2016/05/09)
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- A simple benzimidazole quinoline-conjugate fluorescent chemosensor for highly selective detection of Ag+
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A novel and simple fluorescent chemosensor (L), N-((1H-benzo[d]imidazol-2-yl)methyl)quinoline-2-carboxamide, based on quinoline benzimidazole scaffold was synthesized successfully, which had a ‘turn-on’ effect for Ag+detection in methanol/Tris buffer(1:1, v/v, pH=7.35) and exhibited a strong fluorescence emission at 357?nm (λex=300?nm). The chemosensor had high sensitivity and selectivity for Ag+even in the presence of other metal ions with the detection limit of 4.4×10?7?M, which reached the standard of World Health Organization (WHO) for drinking water (5.0×10?7?M). The mechanism of the interaction between the sensor and Ag+was investigated in detail through NMR and MALDI Mass spectra analysis.
- Chen, Changjun,Liu, Haiyang,Zhang, Bin,Wang, Yanwei,Cai, Kai,Tan, Ying,Gao, Chunmei,Liu, Hongxia,Tan, Chunyan,Jiang, Yuyang
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p. 3980 - 3985
(2016/07/06)
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- Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents
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A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1Hbenzo[ d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.
- Alasmary, Fatmah A.S.,Snelling, Anna M.,Zain, Mohammed E.,Alafeefy, Ahmed M.,Awaad, Amani S.,Karodia, Nazira
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supporting information
p. 15206 - 15223
(2015/09/21)
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- Synthesis and biological evaluation of benzimidazole acridine derivatives as potential DNA-binding and apoptosis-inducing agents
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The discovery of new effective DNA-targeted antitumor agent is needed because of their clinical significance. As acridines can intercalate into DNA and benzimidazoles have the ability to bind in the DNA minor groove, a series of novel benzimidazole acridine derivatives were designed and synthesized to be new DNA-targeted compounds. MTT assay indicated that most of the synthesized compounds displayed good antiproliferative activity, among which compound 8l demonstrated the highest activity against both K562 and HepG-2 cells. Further experiments showed that 8l displayed good DNA-binding capability and inhibited topoisomerase I activity. Moreover, compound 8l could induce apoptosis in K562 cell lines through mitochondrial pathway. These data suggested that compound 8l might be potential as new DNA-binding and apoptosis-inducing antitumor agents.
- Gao, Chunmei,Li, Bin,Zhang, Bin,Sun, Qinsheng,Li, Lulu,Li, Xi,Chen, Changjun,Tan, Chunyan,Liu, Hongxia,Jiang, Yuyang
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p. 1800 - 1807
(2015/03/30)
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- Synthesis and characterization of novel oxadiazole derivatives from benzimidazole
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In the present study, a series of novel N-(1H-benzo[d]imidazol-2-yl)methyl-5-[(hetero)aryl-1,3,4-oxadiazol-2-yl]methanamine (4a-4j) were efficiently synthesized. Condensation of hydrazide derivative 3 with various carboxylic acid derivatives yielded N-[(1H-benzo[d]imidazol-2-yl)methy](5-substituted-1,3,4-oxadiazol-2-yl)methanamine (4a-4j) and compound 5-{[(1H-benzo[d]imidazol-2-yl)methylamino]methyl}-1,3,4-oxadiazole-2-thiol (4k) was obtained on treating hydrazide 3 with carbon disulfide. All the newly synthesized analogues were characterized by IR, 1H NMR, 13C NMR and mass spectral data.
- Vishwanathan, Balasubramanaya,Gurupadayya, Bannimath
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p. 450 - 455
(2015/05/27)
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- Synthesis of benzimidazoles from amino acids with solvent-free melting method
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By using low cost and readily available amino acids as the synthetic blocks, a series of 2-Aminomethyl-benzimidazole are synthesized with solvent-free melting method. While the condensation of aspartic acid (or asparagine) with o-diaminobenzene gives the
- Chen, Ren-Hong,Xiong, Jin-Feng,Peng, Pai,Mo, Guang-Zhen,Tang, Xing-San,Wang, Zhao-Yang,Wang, Xiu-Fang
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p. 926 - 932
(2014/06/09)
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- Design, synthesis, and enzyme kinetics of novel benzimidazole and quinoxaline derivatives as methionine synthase inhibitors
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Methionine synthase catalyzes the transfer of a methyl group from 5-methyltetrahydrofolate to homocysteine, producing methionine and tetrahydrofolate. Benzimidazole and deazatetrahydrofolates derivatives have been shown to inhibit methionine synthase by competing with the substrate 5-methyltetrahydrofolate. In this study, a novel series of substituted benzimidazoles and quinoxalines were designed and assessed for inhibitory activity against purified rat liver methionine synthase using a radiometric enzyme assay. Compounds 3g, 3j, and 5c showed the highest activity against methionine synthase (IC50: 20 μM, 18 μM, 9 μM, respectively). Kinetic analysis of these compounds using Lineweaver-Burk plots revealed characteristics of mixed inhibition for 3g and 5c; and uncompetitive inhibition for 3j. Docking study into a homology model of the rat methionine synthase gave insights into the molecular determinants of the activity of this class of compounds. The identification of these drug-like inhibitors could lead the design of the next generation modulators of methionine synthase.
- Elshihawy, Hosam,Helal, Mohamed A.,Said, Mohamed,Hammad, Mohamed A.
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p. 550 - 558
(2014/01/17)
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- L-Valine-derived simple benzimidazole-based host in selective sensing of Hg(II) ions
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A new and an easy-to-make simple benzimidazole-based chemosensor 1, derived from l-valine is reported. The chemosensor effectively recognises Hg 2+ ion in the open cleft in CH3CN containing 0.2% DMSO by exhibiting significant enhance
- Ghosh, Kumaresh,Sarkar, Tanmay
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p. 748 - 754,7
(2020/09/16)
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- Selective sensing of Cu (II) by a simple anthracene-based tripodal chemosensor
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A new and an easy-to-make simple tripodal shaped chemosensor 1 has been designed and synthesised for metal ions. In CH3CN containing 0.04% DMSO, upon excitation at 370nm, chemosensor 1 exhibited structured emission centred at 418nm, which incre
- Ghosh, Kumaresh,Sarkar, Tanmay
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scheme or table
p. 435 - 440
(2012/01/19)
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- Synthesis and antimicrobial activities of novel peptide deformylase inhibitors
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A new series of N-formylhydroxylamine compounds were designed, optimized with the AutoDock 4.0.1to investigate the interactions between the target compounds and the amino acid residues of the Escherichia coli PDF?Ni enzyme, and then synthesized through mu
- Yin, Ling,Xu, Wei-Ren,Wang, Zhi-Guo,Zhang, Da-Tong,Jia, Jiong,Ge, Yan-Qing,Li, Yan,Wang, Jian-Wu
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experimental part
p. 196 - 205
(2010/10/19)
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- Hybrid NH2-benzimidazole ligands for efficient Ru-catalyzed asymmetric hydrogenation of aryl ketones
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Readily available hybrid NH2/benzimidazole ligands (R-bimaH, 1) dramatically influence the outcome of established Ru-based catalysts during asymmetric hydrogenation of aryl ketones. The benzimidazole functionality results in reversal of the typically observed chiral induction and allows for hydrogenation to be uncharacteristically conducted in nonprotic solvents. The developed systems efficiently catalyzed the AH of a number of ketones in up to 99% ee.
- Li, Yuehui,Ding, Kuiling,Sandoval, Christian A.
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supporting information; experimental part
p. 907 - 910
(2009/07/25)
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- BENZIMIDAZOLE COMPOUNDS THAT ARE VITRONECTIN RECEPTOR ANTAGONISTS
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The present invention provides compounds having formula (I) wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y' each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, -CF3, and -C(O)OH; R, R, R and R are H or specified substituents; R, R, R, R, R, R, R and R are independently selected from H or C1-C3 alkyl; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.
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Page/Page column 22
(2008/06/13)
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- Conversion of the potent δ-opioid agonist H-Dmt-Tic-NH-CH 2-Bid into δ-opioid antagonists by N1-benzimidazole alkylation
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N1-Alkylation of 1H-benzimidizole of the δ agonist H-Dmt-Tic-NH-CH2-Bid with hydrophobic, aromatic, olefinic, acid, ethyl ester, or amide (1-6) became δ antagonists (pA2 = 8.52-10.14). δ- and μ-Opioid receptor affinities w
- Balboni, Gianfranco,Guerrini, Remo,Salvadori, Severo,Negri, Lucia,Giannini, Elisa,Bryant, Sharon D.,Jinsmaa, Yunden,Lazarus, Lawrence H.
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p. 8112 - 8114
(2007/10/03)
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- Synthesis, cytotoxic activity on MCF-7 cell line and mutagenic activity of platinum(II) complexes with 2-substituted benzimidazole ligands
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Four Pt(II) complexes with 2-H/or-methyl/or-aminomethylbenzimidazole or 1,2-dimethylbenzimidazole ligands as "non-leaving groups" were synthesized and their antiproliferative properties were tested against the human MCF-7 breast cancer cell line. The mutagenic potentials of the complexes were tested in Salmonella typhimurium strains TA 98 and TA 100 in the absence of S9 rat liver fraction. In general, Pt(II) complexes tested which were found to be less active than cisplatin, exhibited moderate in vitro cytotoxic activity on MCF-7 cell line. Among the complexes tested, Pt(II) complex with 2-aminomethylbenzimidazole ligand was found to be highly mutagenic in S. typhimurium TA 98 and low mutagenic in S. typhimurium TA 100. Pt(II) complex with 1,2-dimethylbenzimidazole was mutagenic only in S. typhimurium TA 98. The other two complexes were found to be non-mutagen in both strains.
- Guemue, Fatma,Alguel, Oeztekin,Eren, Goekcen,Eroglu, Hatice,Diril, Nuran,Guer, Sibel,Oezkul, Aykut
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p. 473 - 480
(2007/10/03)
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- Benzimidazole compounds that are vitronectin receptor antagonists
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The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d
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- Heterocyclization of the 2-aminoalkyl (and aryl) benzimidazoles under phase transfer catalysis conditions
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A number of new imidazolo (pyrazino and diazepino) benzimidazoles have been prepared by reaction between 2-aminoalkyl (and aryl)benzimidazoles and dibromoalkanes Br-(CH2)n-Br under phase transfer catalysis conditions.These products have been characterized by 1H NMR, IR, MS and their microanalysis. --- Key words: heterocyclization / benzimidazole / diazepinobenzimidazole / benzimidazolo benzodiazepin
- Cherkaoui, O.,Essassi, E.M.,Zniber, R.
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p. 255 - 259
(2007/10/02)
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- Search for non-steroidal anti-inflammatory agents. Part 1: Synthesis of 2-alkyl/aryl-3-benzimidazolylalkylquinazolon-4(3H)-ones.
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Sixteen title compounds have been synthesized and some of them have shown interesting results in antiinflammatory screening against carrageenin-induced inflammation. In addition, the compounds were found to be central nervous system depressants and relatively non-toxic.
- Tiwari,Zaidi,Satsangi
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