title: Inotropic polyazapentalene sulmazole analogues.
abstract: Aryl substituted 1H-imidazo[1,2-a]imidazole 8, imidazo[2,1-b]thiazole 9, 1,4-dihydroimidazo[4,5-d]imidazole 11, and 1(2),4-dihydroimidazo[4,5-c]pyrazoles 12-17 have been prepared. An X-ray crystallographic study confirmed the structure of 8 and showed this analogue to exist as the 1H-tautomer. These heterocycles were evaluated as inotropic agents and analogues 12, 15, and 17 found to display inotropic properties which were less potent in vitro, but more potent in vivo, than those of sulmazole. Structure-activity relationships are discussed.
authors.affiliation: Department of Medicinal Chemistry, Wellcome Research Laboratories, Beckenham, Kent, U.K.
authors.forename: P
authors.initials: P
authors.lastname: Barraclough
authors.forename: J W
authors.initials: JW
authors.lastname: Black
authors.forename: D
authors.initials: D
authors.lastname: Cambridge
authors.forename: D
authors.initials: D
authors.lastname: Firmin
authors.forename: V P
authors.initials: VP
authors.lastname: Gerskowitch
authors.forename: R C
authors.initials: RC
authors.lastname: Glen
authors.forename: H
authors.initials: H
authors.lastname: Giles
authors.forename: J M
authors.initials: JM
authors.lastname: Gillam
authors.forename: R A
authors.initials: RA
authors.lastname: Hull
authors.forename: R
authors.initials: R
authors.lastname: Iyer
mesh_terms: D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004285:Dogs; D006168:Guinea Pigs; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D010210:Papillary Muscles / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D002316:Cardiotonic Agents; D007093:Imidazoles; C029758:sulmazole