Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1, 3, 5-substituted indoles and indazoles

…, TP Maduskuie Jr, HS Shapiro, B Hesp…

Index: Matassa; Maduskuie Jr.; Shapiro; Hesp; Snyder; Aharony; Krell; Keith Journal of Medicinal Chemistry, 1990 , vol. 33, # 6 p. 1781 - 1790

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Citation Number: 92

Abstract

1, 3, 5-Substituted indoles and indazoles have been studied as receptor antagonists of the peptidoleukotrienes. The best of these compounds generally had a methyl group at the N1 position, a [(cyclopentyloxy) carbonyl] amino or 2-cyclopentylacetamido or N'- cyclopentylureido group at the C-5 position, and an arylsulfonyl amide group as part of the acidic chain at the C-3 position of the ring. Such compounds had in vitro dissociation ...