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 ID50 of 0.2 mg/kg in the bronchoconstriction assay.
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Walser et al. (1991) studied this question.
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