Discovery and SAR studies of methionine–proline anilides as dengue virus NS2B-NS3 protease inhibitors

…, Z Weng, X Shao, F Liu, X Nie, J Liu, D Wang…

Index: Zhou, Guo-Chun; Weng, Zhibing; Shao, Xiaoxia; Liu, Fang; Nie, Xin; Liu, Jinsong; Wang, Decai; Wang, Chunguang; Guo, Kai Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6549 - 6554

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Citation Number: 14

Abstract

Abstract A series of methionine–proline dipeptide derivatives and their analogues were designed, synthesized and assayed against the serotype 2 dengue virus NS2B-NS3 protease, and methionine–proline anilides 1 and 2 were found to be the most active DENV 2 NS2B-NS3 competitive inhibitors with K i values of 4.9 and 10.5 μM. The structure and activity relationship and the molecular docking revealed that l-proline, l-methionine and p- ...