Update on SAR Studies Toward New COX-1 Selective Inhibitors.
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.
Paola
P
Vitale
Department of Pharmacy- Pharmaceutical Sciences, University of Bari "Aldo Moro", Bari, Italy. antonio.scilimati@uniba.it.
Antonio
A
Scilimati
Maria Grazia
MG
Perrone
D051545:Cyclooxygenase 1 / Q000737:chemistry / Q000378:metabolism; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry*; D055808:Drug Discovery / Q000639:trends*; D006801:Humans; D013329:Structure-Activity Relationship
D016861:Cyclooxygenase Inhibitors; D051545:Cyclooxygenase 1