| Literature DB >> 21944852 |
Tim Luker1, Roger Bonnert, Steve Brough, Anthony R Cook, Mark R Dickinson, Iain Dougall, Chris Logan, Rukhsana T Mohammed, Stuart Paine, Hitesh J Sanganee, Carol Sargent, Jerzy A Schmidt, Simon Teague, Stephen Thom.
Abstract
Novel indole-3-thio-, 3-sulfonyl- and 3-oxy-aryl-1-acetic acids are reported which are potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). Optimization required maintenance of high CRTh2 potency whilst achieving a concomitant reduction in rates of metabolism, removal of cyp p450 inhibition and minimization of aldose reductase and aldehyde reductase activity. High quality compounds suitable for in vivo studies are highlighted, culminating in the discovery of AZD1981 (22).Entities:
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Year: 2011 PMID： 21944852 DOI： 10.1016/j.bmcl.2011.08.124
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823