title: Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.
abstract: A series of arylpiperazine derivatives were prepared and evaluated for their alpha1-adrenoceptor antagonistic activities and 5alpha-reductase inhibitory activities. SAR study led to the identification of the potent dual-acting compound 2f, which had a pA2 value of 7.5 for alpha1-adrenoceptor antagonism and an IC50 value of 1.5 nM for 5alpha-reductase inhibition.
authors.affiliation: Central Research Laboratories, Zeria Pharmaceutical Co., Ltd., Saitama, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Sato
authors.forename: O
authors.initials: O
authors.lastname: Kitagawa
authors.forename: Y
authors.initials: Y
authors.lastname: Aida
authors.forename: J
authors.initials: J
authors.lastname: Chikazawa
authors.forename: T
authors.initials: T
authors.lastname: Kurimoto
authors.forename: M
authors.initials: M
authors.lastname: Takei
authors.forename: Y
authors.initials: Y
authors.lastname: Fukuta
authors.forename: K
authors.initials: K
authors.lastname: Yoshida
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D042944:Cholestenone 5 alpha-Reductase; D004305:Dose-Response Relationship, Drug; D020128:Inhibitory Concentration 50; D008297:Male; D008956:Models, Chemical; D010088:Oxidoreductases / Q000037:antagonists & inhibitors* / Q000138:chemical synthesis* / Q000494:pharmacology; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D011467:Prostate / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000317:Adrenergic alpha-Antagonists; D010879:Piperazines; D000077489:Piperazine; D010088:Oxidoreductases; D042944:Cholestenone 5 alpha-Reductase