Dual-acting agents with α1-adrenoceptor antagonistic and steroid 5α- reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives

Article abstract of DOI:10.1016/S0960-894X(99)00230-9

A series of arylpiperazine derivatives were prepared and evaluated for their α₁-adrenoceptor antagonistic activities and 5α-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 α₁-adrenoceptor antagonism and an IC₅₀ value of 1.5 nM for 5α-reductase inhibition.