Synthesis and pharmacological evaluation of some DL-dichlorophenyl alcohol amides anticonvulsants.

作者信息

Meza-Toledo Sergio E, Olea-Gómez Arturo, Mora-Ramírez Erika Y, Peralta-Cruz Javier, Noguerón-Chirinos Jaisel B

机构信息

Departamentos de Bioquímica y Química Orgánica, Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional, Prolongación de Carpio y Plan de Ayala, Mexico City, Mexico.

出版信息

Arzneimittelforschung. 2004;54(12):830-4. doi: 10.1055/s-0031-1297037.

The anticonvulsant activity of a homologous series of DL-dichlorophenyl alcohol amides is described. The compounds DL-2-hydroxy-2-(3',4'-dichlorophenyl) butyramide (4, CAS 620950-11-0), DL-3-hydroxy-3-(3',4'-dichlorophenyl) pentanamide (5, CAS 620950-15-4) and DL-4-hydroxy-4-(3',4'-dichlorophenyl) hexanamide (6, CAS 620950-17-6 ) were prepared and tested. Compounds 4, 5 and 6 exhibited a significant activity in seizures induced by pentetrazol. Incorporation of chlorine in the phenyl ring increased their potency. Compound 4 exhibited a slightly lower activity than the reference drug phenobarbital (CAS 50-06-6).