Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373134 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
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.
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Related Topics
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Organic Chemistry
Authors
Martina Hieke, Christine Greiner, Theresa M. Thieme, Manfred Schubert-Zsilavecz, Oliver Werz, Heiko Zettl,