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pubmed-article:2342071pubmed:abstractTextA perception of structural similarities between two independent series of leukotriene antagonists (one emanating from FPL 55712 and one based upon the leukotrienes themselves) led to the discovery of a novel class of indole and indazole derived antagonists of peptidoleukotrienes. A systematic exploration of C-6 substituted 4-(indol-1-ylmethyl)-3-methoxybenzoic acids identified cyclopentylacetamide and cyclopentylurethane as preferred substituents. The corresponding indazoles were equipotent. These compounds are selective leukotriene antagonists with pKB values of 7.5-7.8 vs LTE4 on guinea pig trachea.lld:pubmed
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pubmed-article:2342071pubmed:articleTitleEvolution of a series of peptidoleukotriene antagonists: synthesis and structure-activity relationships of 1,6-disubstituted indoles and indazoles.lld:pubmed
pubmed-article:2342071pubmed:affiliationDepartment of Medicinal Chemistry, ICI Pharmaceuticals Group, Wilmington, Delaware 19897.lld:pubmed
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