Synthesis of 2-phenylbenzofuran derivatives as testosterone 5 alpha-reductase inhibitor |
| |
Authors: | Ishibashi K Nakajima K Sugioka Y Sugiyama M Hamada T Horikoshi H Nishi T |
| |
Institution: | Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan. |
| |
Abstract: | 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 5 alpha-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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|