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A Quantitative Structure-Activity Relationship Study on Some Novel Series of Hydroxamic Acid Analogs Acting as Matrix Metalloproteinase Inhibitors

Sheela Kumaran, Suneel Gupta

Abstract

A quantitative structure-activity relationship study has been made on some pyranyl hydroxamic acid analogs acting as matrix metalloproteinase (MMP) inhibitors. The inhibition potencies of two different series of compounds against two MMP enzymes (MMP-1 and MMP-13) have been analyzed and found to be well correlated with hydrophobic and some indicator parameters of the substituents. In both the cases, hydrophobic parameter of substituents has been found to be a dominant factor. The results of this study led to discuss the selectivity of the compounds for MMP-13 over MMP-1. Keywords: Quantitative structure-activity relationship, matrix metalloproteinase inhibitors, pyranyl hydroxamic acid analogs

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Key concepts: Hydroxamic acid, Matrix metalloproteinase, Matrix metalloproteinase inhibitor, Metalloproteinase, Chemistry, Stereochemistry, Series (stratigraphy), Matrix (chemical analysis)