Design, synthesis, and primary activity evaluation of pyrrolidine derivatives as matrix metalloproteinase inhibitors

J Zhang; X Li; H W Zhu; Q Wang; J H Feng; J J Mou; Y G Li; H Fang; W F Xu

Design, synthesis, and primary activity evaluation of pyrrolidine derivatives as matrix metalloproteinase inhibitors

Drug Discov Ther. 2010 Feb;4(1):5-12.

Authors

J Zhang¹, X Li, H W Zhu, Q Wang, J H Feng, J J Mou, Y G Li, H Fang, W F Xu

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, China.

PMID: 22491146

Abstract

A series of novel pyrrolidine derivatives was designed, synthesized, and assayed to determine the derivatives' activity against matrix metalloproteinase-2 (MMP-2) and aminopeptidase N (APN)/CD13. Preliminary biological tests showed that most compounds inhibit MMP-2 in a highly selective manner compared to APN. Compounds 9d, 9e, and 9g had better inhibitory activity than LY52 and could be used as lead compounds in the future.