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

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

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Bioorganic and Medicinal Chemistry Letters p. 1553 - 1558 (1999)

Update date:2022-08-04

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Authors:

Sato, Hiroki

Kitagawa, Osamu

Aida, Yoshiyuki

Chikazawa, Jun

Kurimoto, Tadashi

Takei, Mineo

Fukuta, Yoshihisa

Yoshida, Kiyoshi

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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.

Full text of DOI:10.1016/S0960-894X(99)00230-9

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