title: Synthesis and antiallergic activity of N-[4-(4-diphenylmethyl-1-piperazinyl)butyl]-1,4-dihydro-4-oxopyridine-3 - carboxamides.
abstract: A new series of oxopyridinecarboxamide derivatives 3a--g and 5a were synthesized and evaluated for their antiallergic activity. 1,4-Dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carboxamides 3a and 5a exhibited potent antiallergic activity (inhibitory rates of 80.7 and 88.3%, respectively, at 20 mg/kg, p.o.) in the rat passive cutaneous anaphylaxis (PCA) test and also exhibited much more potent in vitro inhibitory activity than caffeic acid against the enzyme 5-lipoxygenase (5-LO). Their in vitro antihistamine activity, however, was weaker than that of ketotifen. Compounds 3a and 5a are viewed as promising candidates for antiallergic agents.
authors: Y
authors: Y
authors: Nishikawa
authors: T
authors: T
authors: Shindo
authors: K
authors: K
authors: Ishii
authors: H
authors: H
authors: Nakamura
authors: T
authors: T
authors: Kon
authors: H
authors: H
authors: Uno
authors: J
authors: J
authors: Matsumoto
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004095:Dihydropyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects; D006967:Hypersensitivity / Q000188:drug therapy*; D016859:Lipoxygenase Inhibitors; D008297:Male; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D004095:Dihydropyridines; D016859:Lipoxygenase Inhibitors; D010879:Piperazines