On February 10, 2018, Liu, Sha; Jing, Li; Yu, Zhu-Jun; Wu, Chengyong; Zheng, Yongxiang; Zhang, En; Chen, Qiang; Yu, Yamei; Guo, Li; Wu, Yong; Li, Guo-Bo published an article.COA of Formula: C8H9NO3 The title of the article was ((S)-3-Mercapto-2-methylpropanamido)acetic acid derivatives as metallo-β-lactamase inhibitors: Synthesis, kinetic and crystallographic studies. And the article contained the following:
A set of 2-substituted ((S)-3-mercapto-2-methylpropanamido)acetic acid derivatives I [R = Ph, Bn, 4-HO-C6H4, etc.] were synthesized and some of which displayed potent inhibition with high ligand efficiency to the clin. relevant MBL subtypes, Verona Integron-encoded MBL (VIM)-2 and New Delhi MBL (NDM)-1. Kinetic studies revealed that the inhibitors were not strong zinc chelators in solution, and they bound reversibly to VIM-2 but dissociate very slowly. Crystallog. analyses revealed that they inhibited VIM-2 via chelating the active site zinc ions and interacting with catalytically important residues. Further cell- and zebrafish-based assays revealed that the inhibitors slightly increased the susceptibility of E. coli cells expressing VIM-2 to meropenem and they had no apparent toxicity to the viability of HEK293T cells and the zebrafish embryogenesis. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).COA of Formula: C8H9NO3
The Article related to mercapto alkanamido acetic acid preparation, ndm1 beta lactamase inhibitor antibacterial activity sar mol docking, antibacterial resistance, crystallography, inhibitor design, metallo-β-lactamase (mbl), vim-2 and other aspects.COA of Formula: C8H9NO3
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