Skip to main content

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

Buy Article:

$63.00 plus tax (Refund Policy)

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

Keywords: Anti-inflammatory cytokines; Carbocycles; Cox-1 and Cox-2; Cox-2 Inhibitors; Glucocorticoides; Hetrocycles; Non-Steroidal anti-inflammatory drugs; Vicinal Aryl Moieties

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867003374237

Publication date: November 1, 2000

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
ben/cmc/2000/00000007/00000011/art00002
dcterms_title,dcterms_description,pub_keyword
6
5
20
40
5

Access Key

Free Content
Free content
New Content
New content
Open Access Content
Open access content
Subscribed Content
Subscribed content
Free Trial Content
Free trial content
Cookie Policy
X
Cookie Policy
ingentaconnect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more