Journal of Medicinal Chemistry p. 779 - 782 (1984)
Update date:2022-08-05
Topics:
Clark
Wells
Sansom
et al.
A series of 4-aminobenzamides of some simple primary and secondary amines were prepared and evaluated for anticonvulsant effects. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazole (metrazole) and in the rotorod assay for neurologic deficit. For those N-alkyl amides tested, 4-amino-N-amylbenzamide was the most potent against maximal electroshock seizures (MES): ED50=42.98 mg/kg; however, the N-cyclohexylbenzamide showed the greatest protective index (PI=TD50/ED50), 2.8. The introduction of a second aromatic ring produced more potent compounds, with d,l-4-amino-N-(α-methylbenzyl)-benzamide showing the highest level of activity. This compound has an anti-MES ED50 of 18.02 mg/kg in mice when administered intraperitoneally (ip) and a TD50 of 170.78 mg/kg (PI=9.5) in the same species. These data compare quite favorably with those for phenobarbital and phenytoin in the same assays.
View MoreZhejiang Chemline International Co., Ltd.
Contact:+86-571-88062298
Address:Hengdian Industry Area, Dongyang, Zhejiang, China
lianyungang jinkang pharmaceutical technology co., ltd.
Contact:008651885445517
Address:Jinshan industrial park, Ganyu county, Lianyungang, Jiangsu Province, 222115, China
Jiangsu Cale New Material Co.ltd
Contact:+86-515-88334667/88203550
Address:Zhongshan 3rd Road, Coastal Chemical Industry Park, Yancheng, Jiangsu, China
qingdao goldenchem imp and exp co.,ltd.
Contact:532-55579246
Address:no.62 ,haier road laoshan distirct
Contact:0086-357-6662688
Address:Zhaocheng town, Hongtong County, Linfen City, Shanxi Province
Doi:10.1016/S0040-4039(01)80018-6
(1984)Doi:10.1021/jm00377a012
(1984)Doi:10.1021/acs.orglett.6b01970
(2016)Doi:10.1039/b601412g
(2006)Doi:10.1016/j.carres.2004.05.006
(2004)Doi:10.1246/cl.1984.33
(1984)