title: Studies on cardiotonic agents. V. Synthesis of 1-(6,7-dimethoxy-4-quinazolinyl)piperidine derivatives carrying various 5-membered heterocyclic rings at the 4-position.
abstract: A series of 1-(6,7-dimethoxy-4-quinazolinyl)piperidines carrying various 5-membered heterocycles at the 4-position was synthesized and examined for cardiotonic activity in anesthesized dogs. The (4-oxo-2-thioxo-3-imidazolindinyl)amino derivatives showed the most potent inotropic activity. Marked loss of activity was observed in the 2,4-dihydro-3-thioxo-3H-1,2,4-triazolyl, the 2,4-dihydro-3-oxo-3H-pyrazolyl and the (2,3-dihydro-2-thioxo-3H-1,3,4-thiadiazol-5-yl)amino derivatives. The synthesis and structure-activity relationships are discussed.
authors.affiliation: Pharmaceutical Research Laboratories, Fuji, Kyowa Hakko Kogyo Co., Ltd., Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Nomoto
authors.forename: H
authors.initials: H
authors.lastname: Takai
authors.forename: T
authors.initials: T
authors.lastname: Hirata
authors.forename: M
authors.initials: M
authors.lastname: Teranishi
authors.forename: T
authors.initials: T
authors.lastname: Ohno
authors.forename: K
authors.initials: K
authors.lastname: Kubo
mesh_terms: D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004285:Dogs; D020105:Milrinone; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011728:Pyridones / Q000494:pharmacology
chemical_list: D002316:Cardiotonic Agents; D010880:Piperidines; D011728:Pyridones; D020105:Milrinone