Update on SAR Studies Toward New COX-1 Selective Inhibitors

Author(s): Paola Vitale, Antonio Scilimati, Maria Grazia Perrone

Journal Name: Current Medicinal Chemistry

Volume 22 , Issue 37 , 2015

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Few selective cyclooxygenase-1 (COX-1) inhibitors have been described up to now, although recent studies underlined the involvement of COX-1 in the carcinogenesis, pathogenesis of neuroinflammation, cardiovascular diseases and pain. Among the known COX-1 inhibitors none proved to be a good drug candidate, with the exception of mofezolac, that is clinically used as an analgesic drug. New selective inhibitors were very often discovered as a minor achievement during SAR investigations to discover selective COX-2 inhibitors (COXIBs). After a recognition of the new COX-1 inhibitors synthesized in the last five years, it was attempted to draw, for each chemical class, a structure which might highlight the determinant molecular features able to switch the selectivity towards the COX-1 isoform. Overall, this review could constitute a tool to a better design of novel selective COX-1 inhibitors, to be used in a disease theranostic approach targeting COX-1.

Keywords: Cyclooxygenase (COX)-1, COX-2, structure-activity relationship(SAR), diarylheterocycles, benzanilides, arylpropanoic acids, stilbenes, NSAIDs.

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Article Details

Year: 2015
Published on: 14 December, 2015
Page: [4271 - 4292]
Pages: 22
DOI: 10.2174/0929867322666151029104717
Price: $65

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