title: 2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers.
abstract: Three series of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene and 2-amino-5,6,7,8-tetrahydrocyclohepta[b]thiophenes with 3-carboxylates and carboxamides have been prepared using the Gewald synthesis and evaluated as A(1)AR allosteric enhancers. The structure-activity relationships of these classes of compound are described. A number of compounds, notably 7b, are more potent and efficacious than PD81,723 (1).
authors.affiliation: Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville, Vic. 3052, Australia.
authors.forename: George
authors.initials: G
authors.lastname: Nikolakopoulos
authors.forename: Heidi
authors.initials: H
authors.lastname: Figler
authors.forename: Joel
authors.initials: J
authors.lastname: Linden
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Scammells
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D043682:Receptor, Adenosine A1 / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000577:Amides; D002264:Carboxylic Acids; D043682:Receptor, Adenosine A1; D013876:Thiophenes