Stable analogues of Aminoacyl-tRNA for inhibition of an essential step of bacterial cell-wall synthesis
Stable analogues of Aminoacyl-tRNA for inhibition of an essential step of bacterial cell-wall synthesis
复制标题
DOI：
10.1021/ja0749946
复制
发表时间：
2007-10-24
影响因子：
15
通讯作者：
Etheve-Quelquejeu, Melanie
中科院分区：
文献类型：
--
作者：
Chemama, Maryline;Fonvielle, Matthieu;Etheve-Quelquejeu, Melanie
合成了一种稳定的含有1，2，4恶二唑的Ala-tRNAAla类似物，作为3‘氨基酸酯的MIME，它可以抑制FemX(Wv)，IC50=1.4M-mU)，这是一种丙氨酰转移酶，对于形成革兰氏阳性细菌的肽聚糖网络是必不可少的。恶二唑环是设计核苷酸类似物的一个很好的候选者，它可能适用于包括氨基酰基-tRNA合成酶和核糖体肽转移酶中心在内的重要靶点。
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.