A series of methionine analogues have been synthesized as inhibitors of methionyl-tRNA synthetase and evaluated for their inhibitory activities of E. coli methionyl-tRNA synthetase and bacterial growth. Among them, L-methionine hydroxamate 20 has proved to be the best inhibitor of the enzyme with Ki = 19 microM and showed a growth inhibition against E.coli JM 109, P. vulganis 6059 and C. freundii 8090