Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 5, Pages 1329-1333Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.049
Keywords
Inflammation; Arachidonic acid cascade; SAR; mPGES-1; 5-LO
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Funding
- Aureliasan GmbH (Tuebingen, Germany)
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Dual inhibition of microsomal prostaglandin E-2 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 alpha-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 mu M; IC50 5-LO = 0.1 mu M) showing the most favorable in vitro pharmacological profile. (C) 2011 Elsevier Ltd. All rights reserved.
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