(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity

Journal of Medicinal Chemistry
R A DainesH M Sarau

Abstract

An extensive structure-activity study based around the high-affinity leukotriene B4 (LTB4) receptor antagonist SB 201146 (1) led to the identification of (E)-3-[6-[[(2,6-dichlorophenyl)-thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid (3). This compound displays high affinity for the human neutrophil LTB4 receptor (Ki = 0.78 nM), blocks LTB4-induced Ca2+ mobilization with an IC50 of 6.6 +/- 1.5 nM, and demonstrates potent oral and topical antiinflammatory activity in a murine model of dermal inflammation.

Citations

Dec 22, 2000·Dental Materials : Official Publication of the Academy of Dental Materials·H J Mueller
Dec 2, 2004·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Masayoshi Abe, Tanihiro Yoshimoto
Nov 4, 2004·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Jane R KennyB Kevin Park

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