title: Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists.
abstract: Elaborate study on the three-dimensional model of α(1)-adrenoceptor (α(1)-AR) antagonists led to the development of a series of new arylpiperazine derivatives bearing a flavone nucleus as α(1)-AR antagonists. The in vitro activities were evaluated and compounds 1, 4, 10, 13 and 15 showed activities close to the reference compound (Prazosin).
authors.affiliation: Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
authors.forename: Jing
authors.initials: J
authors.lastname: Jin
authors.forename: Xiao-Bing
authors.initials: XB
authors.lastname: Wang
authors.forename: Ling-Yi
authors.initials: LY
authors.lastname: Kong
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D047309:Flavones / Q000737:chemistry*; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D047309:Flavones; D010879:Piperazines; D018340:Receptors, Adrenergic, alpha-1; C043562:flavone