Design, synthesis and preliminary evaluation of novel pyrrolidine derivatives as matrix metalloproteinase inhibitors.
نویسندگان
چکیده
A series of novel pyrrolidine derivatives were designed, synthesized and assayed for their inhibitory activities on matrix metalloproteinase 2 (MMP-2) and aminopeptidase N (AP-N). The results showed that these pyrrolidine derivatives exhibited highly selective inhibition against MMP-2 as compared with AP-N. The hydroxamates 8a-c were equally or more potent MMP-2 inhibitors than the positive control LY52. The binding mode of the most potent compound 8a with MMP-2 was proposed. Structure-activity relationships were also briefly discussed.
منابع مشابه
Design, synthesis, and primary activity evaluation of pyrrolidine derivatives as matrix metalloproteinase inhibitors.
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 a...
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عنوان ژورنال:
- European journal of medicinal chemistry
دوره 43 10 شماره
صفحات -
تاریخ انتشار 2008