Phenylephrine derivatives as leukotriene D4 antagonists

JH Musser, DM Kubrak, RHW Bender…

Index: Musser, John H.; Kubrak, Dennis M.; Bender, Reinhold H. W.; Kreft, Anthony F.; Nielsen, Susan T.; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 11 p. 2087 - 2093

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Citation Number: 12

Abstract

Two series of phenylephrine derivatives were prepared and tested as inhibitors of leukotriene D4 (LTD4) induced and ovalbumin-induced bronchospasm in the guinea pig. The most potent compound of the urea series,(R)-N, N-diethyl& [2-hydroxy-2-[3-(2- quinolinylmethoxy) phenyl] ethyl]-N-methylurea (3, Wy-47,120), was orally active with ED,'s of 56 mg/kg vs. LTD, and 55 mg/kg vs. ovalbumin. When tested as an antagonist of LTD,- ...