ChemInform Abstract: Dual-Acting Agents with α1-Adrenoceptor Antagonistic and Steroid 5α-Reductase Inhibitory Activities. Synthesis and Evaluation of Arylpiperazine Derivatives.
Cheminform（2010）
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.
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Key words
arylpiperazine derivatives,inhibitory activities,dual-acting
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