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Pentacyclic triazolodiazepines as PAF‐antagonists
Author(s) -
Walser A.,
Flynn T.,
Mason C.
Publication year - 1991
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570280448
Subject(s) - chemistry , bronchoconstriction , antagonist , benzimidazole , stereochemistry , benzodiazepine , pharmacology , biochemistry , receptor , medicine , organic chemistry , asthma
The syntheses of two novel pentacyclic ring systems, the thieno[3,2‐ f ][1,2,4]triazolo[4,3‐ a ][1,4]diazepino‐[4,5‐ a ]benzimidazole and the indazolo[2,3‐ d ][1,2,4]triazolo[4,3‐ a ][1,4]benzodiazepine are described. Attachment of a propargyl linked quinolinone resulted in compounds 6 and 16 which showed PAF‐antagonist activity by the intravenous route of administration in guinea pigs. The more potent compound 16 also exhibited good oral activity with an ID 50 of 0.2 mg/kg in the bronchoconstriction assay.