- Antibacterial studies of copper(I) complexes with benzoylthiourea derivatives
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Four copper(I) complexes of bisbenzoylthiourea derivatives have been synthesized and characterized by elemental analyses as well as IR spectroscopy and TG-DTA analyses. Antibacterial activity assay exhibited MIC50 values of these compounds comp
- Zhao, Meng-Meng,Dong, Xiu-Yan,Yang, Yu-Hua,Li, Gang,Zhang, Yu-Jie,Yang, Xiao-Qin
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Read Online
- Synergism of fused bicyclic 2-aminothiazolyl compounds with polymyxin B against: Klebsiella pneumoniae
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A series of fused bicyclic 2-aminothiazolyl compounds were synthesized and evaluated for their synergistic effects with polymyxin B (PB) against Klebsiella pneumoniae (SIPI-KPN-1712). Some of the synthesized compounds exhibited synergistic activity. When 4 μg ml-1 compound B1 was combined with PB, it showed potent antibacterial activity, achieving 64-fold reduction of the MIC of PB. Furthermore, compound B1 showed prominent synergistic efficacy in both concentration gradient and time-kill curves in vitro. In addition, B1 combined with PB also exhibited synergistic and partial synergistic effect against E. coli (ATCC25922 and its clinical isolates), Acinetobacter baumannii (ATCC19606 and its clinical isolates), and Pseudomonas aeruginosa (Pae-1399).
- Wang, Rong,Hou, Shuang,Dong, Xiaojing,Chen, Daijie,Shao, Lei,Qian, Liujia,Li, Zhong,Xu, Xiaoyong
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supporting information
p. 2060 - 2066
(2017/11/22)
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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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- 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 imidazoline/α2-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies
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Compilation of agmatine structure and imidazoline moiety leads to a new group of imidazoline/α2-adrenoceptor ligands, 4(5)-(2-aminoethyl)imidazoline derivatives. In this study the exploration of previously unknown 4(5)-(2-aminoethyl)imidazolines including the analogues of reported imidazoline and α2-aderenoceptors ligands: clonidine, rilmenidine, idazoxan, efaroxan, antazoline, tracizoline is described. The synthesis of a variety of novel 4(5)-(2-aminoethyl)imidazolines and their I 1, I2, α2-adrenoceptors affinities are reported.
- Treder, Adam P.,Andruszkiewicz, Ryszard,Zgoda, W?odzimierz,Walkowiak, Aleksandra,Ford, Celeste,Hudson, Alan L.
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scheme or table
p. 156 - 167
(2011/03/18)
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- Antimicrobial activity and structural study of disubstituted Thiourea Derivatives
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The antimicrobial activity of six N-phenyl- and fourteen N-benzoylthiourea derivatives were evaluated from their Minimal Inhibitory Concentration (MIC) values using the microdilution procedure against ten microorganisms. Most of the compounds exhibited selective activity against fungi and Gram-positive bacteria, which were very effectively inhibited by some of the tested thioureas. Additionally, SAR considerations and four novel X-ray diffraction structures of N-benzoylthioureas are included. Springer-Verlag 2007.
- Cunha, Silvio,MacEdo Jr., Fernando C.,Costa, Giselle A. N.,Rodrigues Jr., Manoel T.,Verde, Rosival B. V.,De Souza Neta, Lourdes C.,Vencato, Ivo,Lariucci, Carlito,Sa, Fernando P.
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p. 511 - 516
(2008/02/03)
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- Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
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A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 3 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma.
- Das, Jagabandhu,Furch, Joseph A.,Liu, Chunjian,Moquin, Robert V.,Lin, James,Spergel, Steven H.,McIntyre, Kim W.,Shuster, David J.,O'Day, Kathleen D.,Penhallow, Becky,Hung, Chen-Yi,Doweyko, Arthur M.,Kamath, Amrita,Zhang, Hongjian,Marathe, Punit,Kanner, Steven B.,Lin, Tai-An,Dodd, John H.,Barrish, Joel C.,Wityak, John
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p. 3706 - 3712
(2007/10/03)
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- A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential
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The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A2B/A3 antagonist in allergic diseases.
- Press, Neil J.,Taylor, Roger J.,Fullerton, Joseph D.,Tranter, Pamela,McCarthy, Clive,Keller, Thomas H.,Brown, Lyndon,Cheung, Robert,Christie, Julie,Haberthuer, Sandra,Hatto, Julia D.I.,Keenan, Mark,Mercer, Mark K.,Press, Nicola E.,Sahri, Helene,Tuffnell, Andrew R.,Tweed, Morris,Fozard, John R.
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p. 3081 - 3085
(2007/10/03)
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- Pyrimidinone antibiotics - Heterocyclic analogues with improved antibacterial spectrum
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We report the synthesis and pharmacological evaluation of new derivatives of the natural dipeptide antibiotic TAN 1057 A,B containing heterocycles either in the β-amino acid side chain or as mimics of the urea function. In the course of this program, we identified novel analogues that display activity towards a broader panel of Gram-positive bacteriae.
- Brands, Michael,Grande, Yolanda Cancho,Endermann, Rainer,Gahlmann, Reinhold,Krueger, Jochen,Raddatz, Siegfried
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p. 2641 - 2645
(2007/10/03)
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- Substituted N-phenylisothioureas: Potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity
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S-Ethyl N-phenylisothiourea (4) has been found to be a potent inhibitor of both the human constitutive and inducible isoforms of nitric oxide synthase. A series of substituted N-phenylisothiourea analogues was synthesized to investigate the structure-activity relationship of this class of inhibitor. Each analogue was evaluated for human isoform selectivity. One analogue, S-ethyl N-[4-(trifluoromethyl)phenyl]isothiourea (39), exhibited 115-fold and 29-fold selectivity for the neuronal isoform versus the inducible and endothelial derived constitutive isoforms, respectively. Studies have shown the substituted N-phenylisothiourea 39 binds competitively with L,-arginine.
- Shearer, Barry G.,Lee, Shuliang,Oplinger, Jeffrey A.,Frick, Lloyd W.,Garvey, Edward P.,Furfine, Eric S.
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p. 1901 - 1905
(2007/10/03)
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- Improved Procedures for the Preparation of Cycloalkyl-, Arylalkyl-, and Arylthioureas
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An improved procedure for the preparation of arylthioureas consists of the reaction of benzoyl isothiocyanate with anilines in acetone and debenzoylation of the resultant N-aryl-N'-benzoylthioureas with 5percent aqueous sodium hydroxide.Bicycloalkylthioureas and N-(arylalkyl)thioureas (e.g. 9H-9-fluorenylthiourea) are directly prepared from the corresponding isothiocyanates and ammonia.
- Rasmussen, C. R.,Villani, F. J.,Weaner, L. E.,Reynolds, B. E.,Hood, A. R.,et al.
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p. 456 - 459
(2007/10/02)
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