Revista de Ciencias Químicas

Synthesis Of Some Novel C3 Substituted New Diazo-[1,4]-Benzodiazepine-2-One Derivatives As Potent Anticonvulsants

Abstract

Mohd. Rashida, Ravinesh Mishraa, Asif Husaina, Bahar Ahmad

A number of new diazonium salt derivatives of 7-chloro-5-phenyl-3-(phenyl-n-substituted)-diazo-1,3-dihydro-benzo[e][1,4]-diazepin-2-one (IVa-l) from 7-chloro-5-phenyl-1,3-dihydro-benzo[e]-[1,4]-diazepin-2-one (III) with diazonium salts (phenyl diazo salt derivatives) were prepared and tested for anticonvulsant activity. The compounds provided significant protection against maximal electroshock induced seizures (MES) and seizures indicated by sc pentetrazole administration (sc PTZ) at 300 mg/kg after 0.5 h. The compounds IVb, IVd, and IVf were active in MES and sc PTZ indicated seizure. A conformational study of these derivatives was undertaken to explore the mechanistic details of the mode of action and their interlinked, interconvertible and energetically favored geometrical configurations acting on the receptor site.