Journal of Medicinal Chemistry p. 3607 - 3612 (1992)
Update date:2022-08-05
Topics:
Fujioka
Teramoto
Mori
Hosokawa
Sumida
Tominaga
Yabuuchi
A series of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinones has been synthesized and evaluated for positive inotropic activity on the canine heart. Some of these derivatives have a potent activity with none or negative chronotropic effect in isolated, blood-perfused dog heart preparations. They also display a high selectivity for positive inotropic effect over chronotropic and vasodilatory effects in anesthetized dogs. (±)-6-[2- Hydroxy-3-[(3-methoxybenzyl)amino]propoxy]-2(1H)-quinolinone (39) and (±)-6- [3-(3,4-dimethoxybenzyl)amino]-2-hydroxypropoxy]-2(1H)-quinolinone (40) were further investigated in conscious dogs. After iv administration, they did not affect heart rate or mean blood pressure at the dose producing a 50% increase in the peak of the first derivative of the left ventricular pressure. The compounds (39, OPC-18750, and 40, OPC-18790) are the most promising agents with desirable biological activities, and now are currently undergoing clinical evaluation.
View MoreANHUI CHEM-BRIGHT BIOENGINEERING CO.,LTD
Contact:86-561-4080321
Address:No.8 Lieshan Industrial Zone of Huaibei
Contact:+86-021-58123769
Address:No.780 of Cailun Road,Zhangjiang Hi-tech Park,Pudong,Shanghai
website:http://www.afinechem.com
Contact:+86-571-85134551
Address:No. 206 Zhen Hua Road, Hangzhou 310030, Zhejiang, China
Hubei Xinjing New Material Co.,Ltd
Contact:+86-27-83313147
Address:Room402.#Bthe 7th,Headquarter of Huifeng Corporation Qiaokou District,Wuhan China
Reliable Pharma Technology (Shanghai) Co., Ltd.
Contact:0086-21-67676847-8008
Address:Lane 1500, No.68, Xinfei Road, Songjiang District, Shanghai, 201611, P.R.China.
Doi:10.1016/S0040-4039(00)92514-0
(1992)Doi:10.1021/ja01644a014
(1954)Doi:10.1021/ol400578c
(2013)Doi:10.1002/chem.201202528
(2012)Doi:10.1002/chem.201200885
(2012)Doi:10.1039/cc9960001273
(1996)