Affiliation:
1. Departments of Medicinal Chemistry and Inflammatory Diseases Research, Searle Research &
Development, 700 Chesterfield Parkway North, Chesterfield, MO 63198, USA
Abstract
Prostaglandins are synthesized by the enzyme cyclooxygenase (COX), which is the target for nonsteroidal anti-inflammatory drugs (NSAIDs). Recently a second form of COX was discovered (COX-2) that is induced by inflammatory stimuli. The identification of an inducible form of COX led to the hypothesis that COX-2 is responsible for inflammatory prostaglandins, whereas the constitutive COX-I produces physiologically important prostaglandins, e.g., in stomach and kidney. Selective COX- 2 inhibitors have been shown to be anti-inflammatory but do not cause ulcers in the stomach or intestines. It is anticipated that drugs which selectively inhibit COX-2 will be superior anti-inflammatory agents with clear benefits over existing NSAIDs. In this
review, the expression of human COX-I and COX-2 are discussed. A survey of the different chemical classes of COX-2 inhibitors with structure-activity relationships (SAR) and relevant pharmacological profiles are also presented.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology
Cited by
2 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献