Pain and inflammation remain areas of substantial unmet patient need. Current drugs used to treat these conditions have, however, moderate efficacy and can produce a variety of untoward side effects. In this study, we identified a novel hybrid scaffold as a multitarget inhibitor that simultaneously block cyclooxygenase-1 (COX-1), COX-2 and fatty acid amide hydrolase (FAAH). This multitarget strategy may result in improved analgesic efficacy and reduced side effects related to anti-pain drugs, as demonstrated by recent published works (Naidu, et al (2009 ) J Pharmacol Exp Ther 329, 48-56; Fowler, C.J. et al. (2012 ) J Enzym Inhib Med Chem Jan 6; Sasso, et al (2012 ) Pharmacol Res 65, 553). These hybrid compounds are active in the nanomolar range on the three targets, being the most potent multitarget FAAH/COXs inhibitors reported to date. Thus, those compounds may represent promising starting points for the discovery of new analgesic and anti-inflammatory drugs.

Identification of hybrid scaffolds as pontent multitarget FAAH/COX inhibitors

245th National Meeting (2013)

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