The emergence of bacterial strains with resistance to currently marketed antibacterial agents has spurred interest in the
discovery of new antibacterial agents with novel modes of action. One set of potential novel targets are the family of bacterial aminoacyltRNA
synthetases (AaRS). Aminoacyl-tRNA synthetases are the enzymes that catalyze the transfer of amino acids to their cognate tRNA.
They play a pivotal role in protein biosynthesis and are necessary for growth and survival of all cells. Consequently, inhibition of these
enzymes is an attractive target for antibacterial agents. In this review, we examine the latest developments and structure-activity
relationship (SAR) analysis of aminoacyl-tRNA synthetases inhibitors, including methionyl-tRNA synthetase, isoleucyl-tRNA synthetase
and phenylalanyl-tRNA synthetase inhibitors. It is expected that increasing knowledge of the SAR of aminoacyl-tRNA synthetase
inhibitors will be beneficial to the rational design of new generation of antibiotics.
Keywords: Aminoacyl-tRNA synthetases (AaRS), antibacterial agents, methionyl-tRNA synthetase, isoleucyl-tRNA synthetase,
phenylalanyl-tRNA synthetase inhibitors
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