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

Bioorganic & Medicinal Chemistry Letters
2003.0

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.

Knowledge Graph

Similar Paper

Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-Positive antibacterial activity
Bioorganic & Medicinal Chemistry Letters 2003.0
Nanomolar Inhibitors of Staphylococcus aureus Methionyl tRNA Synthetase with Potent Antibacterial Activity against Gram-Positive Pathogens
Journal of Medicinal Chemistry 2002.0
2-[2-Substituted-3-(3,4-dichlorobenzylamino)propylamino]-1H-quinolin-4-ones as Staphylococcus aureus methionyl-tRNA synthetase inhibitors
European Journal of Medicinal Chemistry 2009.0
4-Alkoxy-3-arylfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: Synthesis, molecular docking and antibacterial evaluation
Bioorganic & Medicinal Chemistry 2011.0
Tyrosyl-tRNA synthetase inhibitors as antibacterial agents: Synthesis, molecular docking and structure–activity relationship analysis of 3-aryl-4-arylaminofuran-2(5H)-ones
European Journal of Medicinal Chemistry 2011.0
Synthesis and evaluation of new tyrosyl-tRNA synthetase inhibitors as antibacterial agents based on a N2-(arylacetyl)glycinanilide scaffold
European Journal of Medicinal Chemistry 2015.0
Preparation, antibacterial evaluation and preliminary structure–activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives
Bioorganic & Medicinal Chemistry Letters 2012.0
Design, synthesis and molecular docking of salicylic acid derivatives containing metronidazole as a new class of antimicrobial agents
Bioorganic & Medicinal Chemistry 2015.0
Inhibitors of Bacterial Tyrosyl tRNA Synthetase: Synthesis of Carbocyclic Analogues of the Natural Product SB-219383
Bioorganic & Medicinal Chemistry Letters 2001.0
3-Aryl-4-acyloxyethoxyfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: Synthesis, molecular docking and antibacterial evaluation
Bioorganic & Medicinal Chemistry 2013.0