Ishibashi K, Nakajima K, Sugioka Y, Sugiyama M, Hamada T, Horikoshi H, Nishi T
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Bioorg Med Chem Lett. 1998 Mar 17;8(6):561-6. doi: 10.1016/s0960-894x(98)00001-8.
A series of 2-phenylbenzofuran derivatives with a diphenylmethylcarbamoyl 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. They had inhibitory activities against both enzymes and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl compounds.
合成了一系列在苯并呋喃环的5或6位带有二苯基甲基氨基甲酰基的2-苯基苯并呋喃衍生物，并对其进行了体外大鼠和人睾酮5α-还原酶抑制活性的评估。它们对这两种酶均具有抑制活性，且6-氨基甲酰基衍生物的活性往往比5-氨基甲酰基化合物更强。
