一系列作为细菌苯丙氨酰-tRNA合成酶强效抑制剂的螺环类似物。
A series of spirocyclic analogues as potent inhibitors of bacterial phenylalanyl-tRNA synthetases.
作者信息
Yu Xiang Y, Finn John, Hill Jason M, Wang Zhong G, Keith Dennis, Silverman Jared, Oliver N
机构信息
Department of Medicinal Chemistry, Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
出版信息
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1339-42. doi: 10.1016/j.bmcl.2003.11.081.
We have identified a series of spirocyclic furan and pyrrolidine inhibitors of Enterococcus faecalis and Staphylococcus aureus phenylalanyl-tRNA synthetases. The most potent analogue 1b showed IC50=5 nM (E. faecalis PheRS) and IC50=2 nM (S. aureus PheRS) with high selectivity over the human enzyme. The crystal X-ray structure of analogue 1b was determined.
我们已经鉴定出一系列粪肠球菌和金黄色葡萄球菌苯丙氨酰 - tRNA合成酶的螺环呋喃和吡咯烷抑制剂。最有效的类似物1b对粪肠球菌苯丙氨酰 - tRNA合成酶（IC50 = 5 nM）和金黄色葡萄球菌苯丙氨酰 - tRNA合成酶（IC50 = 2 nM）显示出高效力，并且对人源酶具有高选择性。确定了类似物1b的晶体X射线结构。
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