Update on SAR Studies Toward New COX-1 Selective Inhibitors.

Abstract

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.

• Authors: Paola Vitale, Antonio Scilimati, Maria Grazia Perrone
• Journal: Current medicinal chemistry (Curr Med Chem) Vol. 22 Issue 37 Pg. 4271-92 ( 2015) ISSN: 1875-533X [Electronic] United Arab Emirates
• PMID: 26511468 (Publication Type: Journal Article, Review)

Chemical References

• Cyclooxygenase Inhibitors
• Cyclooxygenase 1

Topics

• Cyclooxygenase 1 (chemistry, metabolism)
• Cyclooxygenase Inhibitors (chemistry)
• Drug Discovery (trends)
• Humans
• Structure-Activity Relationship