一系列新型噻唑作为氨酰-tRNA合成酶抑制剂的合成及其构效关系
Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.
作者信息
Yu X Y, Hill J M, Yu G, Wang W, Kluge A F, Wendler P, Gallant P
机构信息
Department of Medicinal Chemistry, Cubist Pharmaceuticals, Inc., Cambridge, MA 02139, USA.
出版信息
Bioorg Med Chem Lett. 1999 Feb 8;9(3):375-80. doi: 10.1016/s0960-894x(98)00738-0.
Abstract
A series of novel aminoacyl adenylate mimics has been prepared and evaluated for their inhibitory activity against aminoacyl-tRNA synthetases. Several of these thiazole derivatives displayed potent and selective enzyme activity against both Gram-positive and Gram-negative bacteria.
摘要
已经制备了一系列新型氨酰腺苷酸模拟物，并对其针对氨酰 - tRNA合成酶的抑制活性进行了评估。这些噻唑衍生物中的几种对革兰氏阳性菌和革兰氏阴性菌均表现出强效且选择性的酶活性。
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