Synthesis and in vitro enzyme activity of aza, oxa and thia derivatives of bacterial cell wall biosynthesis intermediates

RJ Cox, PSH Wang

文献索引：Cox; Wang Journal of the Chemical Society. Perkin Transactions 1, 2001 , # 17 p. 2022 - 2034

全文：HTML全文

被引用次数: 15

摘要

Mechanism based inhibitors of diaminopimelate aminotransferase (DAP-AT) were designed using knowledge of its substrate specificity and mechanism. Synthesis of thiolester and amide substrate analogues was achieved prior to in vitro inhibition studies, but ester analogues proved too unstable to isolate. Thia substrate analogues showed no inhibitory properties, but the aza substrate analogue 12a showed reversible inhibition vs. DAP-AT ...