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

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

Volume: 7 Issue: 11

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

Affiliation:

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.

Cite this article as:

Dannhardt G. and Laufer S., Structural Approaches to Explain the Selectivity of COX-2 Inhibitors: Is There a Common Pharmacophore?, Current Medicinal Chemistry 2000; 7 (11) . https://dx.doi.org/10.2174/0929867003374237