80937-24-2Relevant academic research and scientific papers
Design, synthesis, and bioevaluation of a novel class of (E)-4-oxo-crotonamide derivatives as potent antituberculosis agents
Ren, Jinfeng,Xu, Jian,Zhang, Guoning,Xu, Changliang,Zhao, LiLi,You, XueFu,Wang, Yucheng,Lu, Yu,Yu, Liyan,Wang, Juxian
supporting information, p. 539 - 543 (2019/01/09)
A series of novel (E)-4-oxo-2-crotonamide derivatives were designed and synthesized to find potent antituberculosis agents. All the target compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv(MTB). Results reveal that 4-phenyl moiety at part A and short methyl group at part C were found to be favorable. Most of the derivatives displayed promising activity against MTB with MIC ranging from 0.125 to 4 μg/mL. Especially, compound IIIa16 was found to have the best activity with MIC of 0.125 μg/mL against MTB and with MIC in the range of 0.05–0.48 μg/mL against drug-resistant clinical MTB isolates.
CoA adducts of 4-oxo-4-phenylbut-2-enoates: Inhibitors of MenB from the M. tuberculosis menaquinone biosynthesis pathway
Li, Xiaokai,Liu, Nina,Zhang, Huaning,Knudson, Susan E.,Li, Huei-Jiun,Lai, Cheng-Tsung,Simmerling, Carlos,Slayden, Richard A.,Tonge, Peter J.
supporting information; experimental part, p. 818 - 823 (2012/01/06)
A high-throughput screen led to the discovery of 2-amino-4-oxo-4- phenylbutanoate inhibitors of the 1,4-dihydroxy-2-naphthoyl-CoA synthase (MenB) from the menaquinone biosynthesis pathway in Mycobacterium tuberculosis. However, these compounds are unstabl
First total synthesis of the antifungal antibiotic thiobutacin
Chakor, Narayan,Dallavalle, Sabrina,Musso, Loana,Moretti, Maddalena
, p. 5056 - 5058 (2008/12/20)
The first total synthesis of thiobutacin, a butanoic acid with antifungal activity recently isolated from the culture broth of a soil actinomycete, Lechevalieria aerocolonigenes strain VK-A9, is described. The five-step procedure involves readily availabl
Novel human lens metabolites from normal and cataractous human lenses
Mizdrak, Jasminka,Hains, Peter G.,Kalinowski, Danuta,Truscott, Roger J.W.,Davies, Michael J.,Jamie, Joanne F.
, p. 4990 - 4999 (2008/02/01)
4-(2-Aminophenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid and glutathionyl-kynurenine have been identified as novel metabolites in normal and cataractous human lenses following total synthesis and comparison with authentic human
N-(4-(PIPERAZIN-1-YL)-PHENYL-2-OXAZOLIDINONE-5-CARBOXAMIDE DERIVATES AND RELATED COMPOUNDS AS ANTIBACTERIAL AGENTS
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Page/Page column 127, (2010/02/07)
The present invention provides antibacterial agents having the formula I described herein. or-pharmaceutically acceptable salts thereof wherein: A is a structure i, ii, iii, or iv,W is N(H)C(X)-R,. Het, or -Y HET, in which the Hot or Y HET is option
