Chemical and Pharmaceutical Bulletin p. 333 - 337 (1997)
Update date:2022-09-26
Topics:
Okada, Minoru
Yoden, Toru
Kawaminami, Eiji
Shimada, Yoshiaki
Kudoh, Masafumi
Isomura, Yasuo
1-N,N-Disubstituted amino-1H-1,2,4-triazole derivatives were prepared and evaluated for aromatase-inhibitory activity (in vitro) and for the inhibitory activity on pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis (in vivo). 1-N-para-Substituted benzylamino derivatives, having an electron-withdrawing group on the phenyl moiety, exhibited aromatase-inhibitory activity in vitro and in vivo. Among them, 1-[(4- nitrobenzyl)(4-nitrophenyl)amino]-1H-1,2,4-triazole (5b) was the most potent aromatase inhibitor. These 1-N-benzylamino derivatives also showed relatively strong inhibitory activity on aldosterone synthesis, indicating that the selectivity of these derivatives for aromatase inhibition was not sufficient in comparison with that of the 4-amino-4H-1,2,4-triazole derivatives.
View MoreShanghai ZaiQi Bio-Tech Co., Ltd.,
Contact:+86-21-5482 4098
Address:Bldg. No.7, No.201 MinYi Rd，Songjiang CaoHeJing High-Tech Park Shanghai 201516 P,R,China
SEA BRGIHT INDUSTRY CO.,LIMITED
Contact:0086 755 8622 3990
Address:Rm 17B3,GuangCaiXinTianDi Bldg,GuiMiao Rd,NanShan District,Shenzhen,China
Contact:+86-27-67841589
Address:Add: 999 Gaoxin Road, Donghu New Technology Development Zone, Wuhan City, Hubei, China
Taizhou YOJOY Chemical Co., Ltd.
Contact:13857143241
Address:Yangfu Industrial Park, Xianju, Zhejiang, P. R. China
Shantou Baokang Pharmaceutical Co., Ltd.
Contact:+86-754-88873487
Address:5/F B Block Huangshan Bldg Huangshan Rd Shantou
Doi:10.1021/ja047556x
(2004)Doi:10.1016/S0040-4020(97)00560-7
(1997)Doi:10.1002/(SICI)1522-2675(19991215)82:12<2231::AID-HLCA2231>3.0.CO;2-Z
(1999)Doi:10.1016/j.bmc.2005.02.060
(2005)Doi:10.1021/jo402212j
(2013)Doi:10.1021/ja00067a023
(1993)
