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 Golden-Shell Pharmaceutical Co.,Ltd.
Contact:+86-576-87501888 / 87501988
Address:No.89 Zhongxing Road. Li'ao, Yuhuan, Zhejiang, China
NEW FORTUNE INDUSTRIAL CO.,LTD.
website:http://newfortune.lookchem.com/
Contact:+86-25-8645-9456
Address:C4-105 GREEN ISLAND FLOWER TOWN
Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd
website:http://www.jlpharms.com
Contact:+86-571-86982636
Address:Rm A606, Fuyi Center, jianqiao street, Jianggan Area
website:http://www.shochem.com
Contact:021-50800795
Address:No.1043, Halei Rd, Zhangjiang Hi-Tech Park, Shanghai, Postcode 201203, China
Suzhou HeChuang Chemical Co.,Ltd.
Contact:+86-512-88800520
Address:No.9 Guanchao Rd,Changshu Advanced Materials Industy Park
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)