Structural approaches to explain the selectivity of COX-2 inhibitors: is there a common pharmacophore?

Abstract:

:The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient non-steroidal 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.

journal_name

Curr Med Chem

authors

Dannhardt G,Laufer S

doi

10.2174/0929867003374237

subject

Has Abstract

pub_date

2000-11-01 00:00:00

pages

1101-12

issue

11

eissn

0929-8673

issn

1875-533X

journal_volume

7

pub_type

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