Bioorganic and Medicinal Chemistry Letters p. 1553 - 1558 (1999)
Update date:2022-08-04
Topics:
Sato, Hiroki
Kitagawa, Osamu
Aida, Yoshiyuki
Chikazawa, Jun
Kurimoto, Tadashi
Takei, Mineo
Fukuta, Yoshihisa
Yoshida, Kiyoshi
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.
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(1999)