Stable analogues of Aminoacyl-tRNA for inhibition of an essential step of bacterial cell-wall synthesis

被引:27
作者
Chemama, Maryline
Fonvielle, Matthieu
Villet, Regis
Arthur, Michel
Valery, Jean-Marc
Etheve-Quelquejeu, Melanie
机构
[1] Univ Paris 06, CNRS, UMR 7613, Paris, France
[2] INSERM, LRMA, Ctr Rech Cordeliers, U8722,Equipe 12, F-75006 Paris, France
[3] Univ Paris 06, UMR S 872, F-75006 Paris, France
[4] Univ Paris 05, UMR S 872, F-75006 Paris, France
关键词
D O I
10.1021/ja0749946
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:12642 / +
页数:3
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