Document Report Card

Basic Information

ID: ALA1131733

Journal: Bioorg Med Chem Lett

Title: Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.

Authors: Sato H, Kitagawa O, Aida Y, Chikazawa J, Kurimoto T, Takei M, Fukuta Y, Yoshida K.

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.

CiteXplore: 10386934

DOI: 10.1016/s0960-894x(99)00230-9