Literature DB >> 12639554

Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity.

Richard L Jarvest1, John M Berge, Murray J Brown, Pamela Brown, John S Elder, Andrew K Forrest, C S V Houge-Frydrych, Peter J O'Hanlon, David J McNair, Stephen Rittenhouse, Robert J Sheppard.   

Abstract

Optimisation of the left-hand-side aryl moiety of a file compound screening hit against Staphylococcus aureus methionyl tRNA synthetase led to the identification of a series of potent nanomolar inhibitors. The best compounds showed excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics.

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Year:  2003        PMID： 12639554     DOI： 10.1016/s0960-894x(02)01027-2

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


  10 in total

1.  Selective inhibitors of methionyl-tRNA synthetase have potent activity against Trypanosoma brucei Infection in Mice.

Authors:  Sayaka Shibata; J Robert Gillespie; Angela M Kelley; Alberto J Napuli; Zhongsheng Zhang; Kuzma V Kovzun; Ranae M Pefley; Jocelyn Lam; Frank H Zucker; Wesley C Van Voorhis; Ethan A Merritt; Wim G J Hol; Christophe L M J Verlinde; Erkang Fan; Frederick S Buckner
Journal:  Antimicrob Agents Chemother       Date:  2011-01-31       Impact factor: 5.191

2.  Inhibition of methionyl-tRNA synthetase by REP8839 and effects of resistance mutations on enzyme activity.

Authors:  Louis S Green; James M Bullard; Wendy Ribble; Frank Dean; David F Ayers; Urs A Ochsner; Nebojsa Janjic; Thale C Jarvis
Journal:  Antimicrob Agents Chemother       Date:  2008-11-17       Impact factor: 5.191

3.  Prediction of protein crystallization outcome using a hybrid method.

Authors:  Frank H Zucker; Christine Stewart; Jaclyn dela Rosa; Jessica Kim; Li Zhang; Liren Xiao; Jenni Ross; Alberto J Napuli; Natascha Mueller; Lisa J Castaneda; Stephen R Nakazawa Hewitt; Tracy L Arakaki; Eric T Larson; Easwara Subramanian; Christophe L M J Verlinde; Erkang Fan; Frederick S Buckner; Wesley C Van Voorhis; Ethan A Merritt; Wim G J Hol
Journal:  J Struct Biol       Date:  2010-03-27       Impact factor: 2.867

4.  Antibacterial activity of REP8839, a new antibiotic for topical use.

Authors:  Ian A Critchley; Casey L Young; Kimberley C Stone; Urs A Ochsner; Joseph Guiles; Ted Tarasow; Nebojsa Janjic
Journal:  Antimicrob Agents Chemother       Date:  2005-10       Impact factor: 5.191

5.  Mode of action and biochemical characterization of REP8839, a novel inhibitor of methionyl-tRNA synthetase.

Authors:  Urs A Ochsner; Casey L Young; Kimberley C Stone; Frank B Dean; Nebojsa Janjic; Ian A Critchley
Journal:  Antimicrob Agents Chemother       Date:  2005-10       Impact factor: 5.191

6.  Development of Methionyl-tRNA Synthetase Inhibitors as Antibiotics for Gram-Positive Bacterial Infections.

Authors:  Omeed Faghih; Zhongsheng Zhang; Ranae M Ranade; J Robert Gillespie; Sharon A Creason; Wenlin Huang; Sayaka Shibata; Ximena Barros-Álvarez; Christophe L M J Verlinde; Wim G J Hol; Erkang Fan; Frederick S Buckner
Journal:  Antimicrob Agents Chemother       Date:  2017-10-24       Impact factor: 5.191

7.  Structure of Leishmania major methionyl-tRNA synthetase in complex with intermediate products methionyladenylate and pyrophosphate.

Authors:  Eric T Larson; Jessica E Kim; Frank H Zucker; Angela Kelley; Natascha Mueller; Alberto J Napuli; Christophe L M J Verlinde; Erkang Fan; Frederick S Buckner; Wesley C Van Voorhis; Ethan A Merritt; Wim G J Hol
Journal:  Biochimie       Date:  2010-12-07       Impact factor: 4.079

8.  Fragment screening and structural analyses highlight the ATP-assisted ligand binding for inhibitor discovery against type 1 methionyl-tRNA synthetase.

Authors:  Jia Yi; Zhengjun Cai; Haipeng Qiu; Feihu Lu; Zhiteng Luo; Bingyi Chen; Qiong Gu; Jun Xu; Huihao Zhou
Journal:  Nucleic Acids Res       Date:  2022-04-26       Impact factor: 19.160

Review 9.  Aminoacyl-tRNA synthetases as drug targets in eukaryotic parasites.

Authors:  James S Pham; Karen L Dawson; Katherine E Jackson; Erin E Lim; Charisse Flerida A Pasaje; Kelsey E C Turner; Stuart A Ralph
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2013-11-11       Impact factor: 4.077

10.  Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis.

Authors:  Kayode K Ojo; Ranae M Ranade; Zhongsheng Zhang; David M Dranow; Janette B Myers; Ryan Choi; Steve Nakazawa Hewitt; Thomas E Edwards; Douglas R Davies; Donald Lorimer; Stephen M Boyle; Lynn K Barrett; Frederick S Buckner; Erkang Fan; Wesley C Van Voorhis
Journal:  PLoS One       Date:  2016-08-08       Impact factor: 3.240
  10 in total

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