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 MoreShanghai Rechem Science Co., Ltd.
website:http://www.rechemscience.com/
Contact:+86-21-51623867
Address:Shanghai
Hangzhou Sartort Biopharma Co., Ltd
website:http://www.sartort.com
Contact:86-571-87039693
Address:No. 57, Tech Park Road, Hangzhou, Zhejiang, China
Yangling Ciyuan biotech Co., Ltd.
Contact:86-15802970736
Address:2-1804, International Park Mansion, No.2, South Fengdeng Road, Lianhu District
Ji'nan Orgachem Pharmaceutical Co.,Ltd
Contact:+86-531-82687810
Address:Jinan
Hubei Xinghuo Chemical Co., Ltd.,
Contact:13925817279 13907299441
Address:Xinghuo Fine Chemistry Industrial Park, Xiaochang County, Hubei Province, 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)