Chemical and Pharmaceutical Bulletin p. 899 - 906 (1992)
Update date:2022-09-26
Topics:
Take
Okumura
Takimoto
Ohtsuka
Shiokawa
A series of 1,1'-biphenyl-2,6-dicarboxylic acid diesters with an aminoalkyl group in the ester function were synthesized and examined for their inhibitory activity on detrusor contraction in vitro and in vivo. In the in vivo test, arrhythmia was observed as a side effect. Among those compounds synthesized, 2-methyl 6-[4-(1-methylpiperidinyl)] 3-hydroxy-5-methyl-2'-nitro-1,1'-biphenyl-2,6-dicahboxylate (18) showed strong inhibitory activity on detrusor contractions in vivo (ED50 = 0.54 mg/kg i.v., ED50 = 7.2 mg/kg i.d.) and good separation from the side effect. Compound 18 was chosen for further pharmacological evaluation as an agent for the treatment of overactive detrusor.
View MoreContact:+33-5-34012600
Address:28 ZA des Pignès
website:https://www.finerchem.com
Contact:+86-531-88989536
Address:New Material Industrial Park, Jinan City, China
Hefei Highzone Fine Chemical S&T CO.,LTD
Contact:86-0551-63663560
Address:room 1801 NO. 24 Shuguang RD.
Dalian Join King Biochemical Tech. Co., Ltd.
Contact:0411 39216206
Address:814 First State Blvd
website:http://www.cartoonchem.com/
Contact:+86-25-58074918
Address:Room 2109, RuiHua Business Center,315 South ZhongShan Road, Nanjing 210001, China
Doi:10.1016/j.dyepig.2013.02.005
(2013)Doi:10.1016/j.bmc.2013.01.038
(2013)Doi:10.1016/j.ejmech.2012.11.033
(2013)Doi:10.1021/cn500330v
(2015)Doi:10.1002/cjoc.201180343
(2011)Doi:10.1016/j.bmcl.2012.06.072
(2012)
