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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Structural Approaches to Explain the Selectivity of COX-2 Inhibitors: Is There a Common Pharmacophore?

Author(s): G. Dannhardt and S. Laufer

Volume 7 , Issue 11 , 2000

Page: [1101 - 1112] Pages: 12

DOI: 10.2174/0929867003374237

Price: $65

Abstract

The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient nonsteroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five structural classes can be identified together with a class bearing little or no resemblance to one another in their molecular structure. The most interesting point is the very distinct structure/activity relationship. On the one hand only minor modifications to a particular compound induce a drastic change in its COX selectivity and on the other hand the structural prerequisites in terms of molecular shape, lipophilicity, electron density, flexibility, polarity and H-bonding dynamics allow a wide range of diversity.


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