Chemical and Pharmaceutical Bulletin · 1982 · 18 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyGeneral PharmacologyStructure-activity RelationshipsSynthetic Medicinal ChemistryHeterocyclic ChemistryStructure-activity Relationship AnalysisAbsolute PotencyMedicinal HeterocyclesPassive Cutaneous AnaphylaxisPolycyclic HeterocyclesPyridine Chemistry
A series of phenyl-substituted pyrones, pyridines, and pyrimidines bearing a 5-tetrazolyl or N-(5-tetrazolyl) carbamoyl group as an acidic moiety was synthesized. The compounds were tested for antiallergic activity by passive cutaneous anaphylaxis (PCA) assay in rats after oral administration. Among the compounds synthesized. N-(5-tetrazolyl)-6-phenylpyridine-2-carboxamides (53, 54 and 55) were found to display remarkably high potency.