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

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

Zhang J, Li X, Zhu HW, Wang Q, Feng JH, Mou JJ, Li YG, Fang H, Xu WF


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.

KEYWORDS: Matrix metalloproteinase-2, aminopeptidase N, inhibitors, pyrrolidine derivatives, synthesis

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