Literature DB >> 12798340

Discovery of a potent and selective series of pyrazole bacterial methionyl-tRNA synthetase inhibitors.

John Finn1, Karen Mattia, Mike Morytko, Siya Ram, Yingfei Yang, Ximao Wu, Elsa Mak, Paul Gallant, Dennis Keith.   

Abstract

Starting with a micromolar lead identified from high-throughput screening, a series of pyrazoles were discovered with significantly improved potency on bacterial methionyl-tRNA synthetase and selectivity over human methionyl-tRNA synthetase.

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Year:  2003        PMID： 12798340     DOI： 10.1016/s0960-894x(03)00298-1

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


  6 in total

1.  IA, database of known ligands of aminoacyl-tRNA synthetases.

Authors:  Mieczyslaw Torchala; Marcin Hoffmann
Journal:  J Comput Aided Mol Des       Date:  2007-09-20       Impact factor: 3.686

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.  A homology model for Clostridium difficile methionyl tRNA synthetase: active site analysis and docking interactions.

Authors:  Ehab Al-Moubarak; Claire Simons
Journal:  J Mol Model       Date:  2010-11-02       Impact factor: 1.810

4.  Discovering new classes of Brugia malayi asparaginyl-tRNA synthetase inhibitors and relating specificity to conformational change.

Authors:  Sai Chetan K Sukuru; Thibaut Crepin; Youli Milev; Liesl C Marsh; Jonathan B Hill; Regan J Anderson; Jonathan C Morris; Anjali Rohatgi; Gavin O'Mahony; Morten Grøtli; Franck Danel; Malcolm G P Page; Michael Härtlein; Stephen Cusack; Michael A Kron; Leslie A Kuhn
Journal:  J Comput Aided Mol Des       Date:  2006-04-28       Impact factor: 3.686

5.  Novel [l,2,4]triazolo[3,4-a]isoquinoline chalcones as new chemotherapeutic agents: Block IAP tyrosine kinase domain and induce both intrinsic and extrinsic pathways of apoptosis.

Authors:  Magda F Mohamed; Farid M Sroor; Nada S Ibrahim; Ghada S Salem; Hadeer H El-Sayed; Marwa M Mahmoud; Menna-Allah M Wagdy; Amina M Ahmed; Aya-Allah T Mahmoud; Somia S Ibrahim; Mariam M Ismail; Sanaa Mohy Eldin; Fatma M Saleh; Hamdi M Hassaneen; Ismail A Abdelhamid
Journal:  Invest New Drugs       Date:  2020-08-28       Impact factor: 3.850

Review 6.  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
  6 in total

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