Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl) oxy] methyl] acetophenone derivatives

…, D McCullough, KD Haisch, LE Rinkema…

Index: Dillard, Robert D.; Carr, F. Patrick; McCullough, Doris; Haisch, Klaus D.; Rinkema, Lynn E.; Fleisch, Jerome H. Journal of Medicinal Chemistry, 1987 , vol. 30, # 5 p. 911 - 918

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Citation Number: 25

Abstract

A series of [[(tetrazol-5-ylaryl) oxy] methyl] acetophenones was synthesized and evaluated as antagonists of leukotriene D4 induced contractions of guinea pig ileum. Substitutions at the 3-position of the acetophenone with ethyl (66), propyl (68), butyl (83), and isobutyl (84) gave-log IC5o values of 7.9, 8.0, 7.8, and 7.7, respectively. Equally potent compounds were obtained when the tetrazol-5-yl group was connected to the second benzene ring in the ...