Jm. Berge et al., Synthesis and activity of analogues of SB-219383: Novel potent inhibitors of bacterial tyrosyl tRNA synthetase, J ANTIBIOT, 53(11), 2000, pp. 1282-1292
SB-219383 is a naturally occurring antibiotic, which acts by inhibition of
tyrosyl tRNA synthetase. Semi-synthetic derivatives of SB-219383 were prepa
red with the objective of elucidating the key features required for inhibit
ion of tyrosyl tRNA synthetase in order to improve the antibacterial activi
ty. Some ester and amide derivatives as well as monocyclic analogues exhibi
ted sub-nanomolar inhibitory activity against tyrosyl tRNA synthetase.