Design, Synthesis, and Evaluation of a Pyrrolinone-Based Matrix Metalloprotease Inhibitor

A pyrrolinone-based hydroxamate matrix metalloprotease inhibitor, (−)-1, has been designed and synthesized. Enzymatic assay revealed that (−)-1 inhibited three of the ten matrix metalloprotease enzymes examined and as such represents a new, potentially important lead structure.

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Bibliographic Details
Published in:Organic letters 2000-11, Vol.2 (24), p.3809-3812
Main Authors: Smith, Amos B, Nittoli, Thomas, Sprengeler, Paul A, Duan, James J.-W, Liu, Rui-Qin, Hirschmann, Ralph F
Format: Article
Language:English
Subjects:
Aldehydes
Drug Design
Isoenzymes - antagonists & inhibitors
Metalloendopeptidases - antagonists & inhibitors
Metalloendopeptidases - chemistry
Models, Molecular
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Pyrroles - chemical synthesis
Pyrroles - chemistry
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Description
Summary:A pyrrolinone-based hydroxamate matrix metalloprotease inhibitor, (−)-1, has been designed and synthesized. Enzymatic assay revealed that (−)-1 inhibited three of the ten matrix metalloprotease enzymes examined and as such represents a new, potentially important lead structure.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol000254p