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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Author(s): S. P. Gupta, Priyanka Bagaria and V. S.A. Kumar Satuluri

Volume 5, Issue 4, 2008

Page: [281 - 285] Pages: 5

DOI: 10.2174/157018008784619852

Price: $65

Abstract

A Quantitative structure-activity relationship study (QSAR) has been made on a novel series of hydroxamic acid-based matrix metalloproteinase (MMP) inhibitors. The inhibition potencies of the compounds against two MMPs, MMP-2 and MMP-3, are found to be significantly correlated with Kiers first-order valence molecular connectivity index (1xv) and Hammetts electronic constant of the substituents. It is thus found that in addition to zinc-binding group of inhibitors interacting with the zinc ion present in the MMPs, some other groups also in the molecules may have some sorts of physicochemical interactions with the sub-sites of MMPs

Keywords: Quantitative structure-activity relationship, Matrix metalloproteinase inhibitors, Hydroxamic acids


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