Journal of the American Chemical Society, Vol.129, No.42, 12642-12642, 2007
Stable analogues of Aminoacyl-tRNA for inhibition of an essential step of bacterial cell-wall synthesis
A stable analogue of Ala-tRNAAla containing 1,2,4 oxadiazole as a mime of the 3' amino acyl ester was synthesized and showed to inhibit FemX(wv), IC50 = 1.4 M-mu), an alanyl transferase essential to form the peptidoglycan network of Gram-positive bacteria] pathogens. The oxadiazole ring is a good candidate for design of nucleotide analogues which may be applicable to important targets including amino acyl-tRNA synthetases and the ribosomal peptidyl-transferase center.