1287678-07-2Relevant academic research and scientific papers
A novel class of dual mPGES-1/5-LO inhibitors based on the α-naphthyl pirinixic acid scaffold
Hieke, Martina,Greiner, Christine,Thieme, Theresa M.,Schubert-Zsilavecz, Manfred,Werz, Oliver,Zettl, Heiko
, p. 1329 - 1333 (2011/04/16)
Dual inhibition of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO) represents a promising strategy in the development of novel anti-inflammatory drugs targeting the arachidonic acid cascade. Herein, a class of α-naphthyl pirinixic acids is characterized as dual mPGES-1/5-LO inhibitors. Systematic structural variation was focused on the lipophilic backbone of the scaffold and yielded detailed structure-activity relationships (SAR) with compound 16 (IC50 mPGES-1 = 0.94 μM; IC50 5-LO = 0.1 μM) showing the most favorable in vitro pharmacological profile.
