222308-72-7Relevant academic research and scientific papers
Synthesis of 2-phenylbenzofuran derivatives as testosterone 5α- reductase inhibitor
Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Sugiyama, Mitsuo,Hamada, Takakazu,Horikoshi, Hiroyoshi,Nishi, Takahide
, p. 226 - 240 (1999)
A series of 2-phenylbenzofuran derivatives with a carbamoyl, alkylamino, or alkyloxy group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5α-reductase inhibitory activities in vitro. Against rat enzyme, the carbamoyl derivatives had more potent inhibitory activities than the alkylamino or alkyloxy derivatives, and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl derivatives. Against human enzyme, the 6-substituted derivatives had more potent inhibitory activities than the 5-substituted derivatives. The 6-carbamoyl and 6-alkylamino derivatives tended to show stronger inhibitory activities against human type 1 enzyme than against type 2 enzyme, but they were not largely selective.
