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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