Literature DB >> 14980694

A series of spirocyclic analogues as potent inhibitors of bacterial phenylalanyl-tRNA synthetases.

Xiang Y Yu1, John Finn, Jason M Hill, Zhong G Wang, Dennis Keith, Jared Silverman, N Oliver.   

Abstract

We have identified a series of spirocyclic furan and pyrrolidine inhibitors of Enterococcus faecalis and Staphylococcus aureus phenylalanyl-tRNA synthetases. The most potent analogue 1b showed IC50=5 nM (E. faecalis PheRS) and IC50=2 nM (S. aureus PheRS) with high selectivity over the human enzyme. The crystal X-ray structure of analogue 1b was determined.

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Year:  2004        PMID: 14980694     DOI: 10.1016/j.bmcl.2003.11.081

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  High Throughput Screen Identifies Natural Product Inhibitor of Phenylalanyl-tRNA Synthetase from Pseudomonas aeruginosa and Streptococcus pneumoniae.

Authors:  Yanmei Hu; Stephanie O Palmer; Hector Munoz; James M Bullard
Journal:  Curr Drug Discov Technol       Date:  2014

2.  The role of a novel auxiliary pocket in bacterial phenylalanyl-tRNA synthetase druggability.

Authors:  Ayome Abibi; Andrew D Ferguson; Paul R Fleming; Ning Gao; Laurel I Hajec; Jun Hu; Valerie A Laganas; David C McKinney; Sarah M McLeod; D Bryan Prince; Adam B Shapiro; Ed T Buurman
Journal:  J Biol Chem       Date:  2014-06-16       Impact factor: 5.157

3.  Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy.

Authors:  Puay-Wah Phuan; Guido Veit; Joseph Tan; Ariel Roldan; Walter E Finkbeiner; Gergely L Lukacs; A S Verkman
Journal:  Mol Pharmacol       Date:  2014-04-15       Impact factor: 4.436

Review 4.  Recent applications of ninhydrin in multicomponent reactions.

Authors:  Suven Das
Journal:  RSC Adv       Date:  2020-05-18       Impact factor: 4.036

Review 5.  Evolutionary Limitation and Opportunities for Developing tRNA Synthetase Inhibitors with 5-Binding-Mode Classification.

Authors:  Pengfei Fang; Min Guo
Journal:  Life (Basel)       Date:  2015-12-08
  5 in total

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