Application of Topliss Modified Approach in the Design and Synthesis of GABA-Nergic Anticonvulsants Sawant RL1,*, Bhatia MS2 1P.D.V.V.P.F's College of Pharmacy, Vilad Ghat, Post MIDC, Ahmednagar – 414 111 (M.S.) 2Bharti Vidyapeeth's College of Pharmacy, Near Chitranagari, Kolhapur – 416 013 (M. S.) *Corresponding Author E-mail: sawantrl@yahoo.com
Abstract (14Z)-8-(4-Substituted phenyl) dibenzo[1,2,4]triazolo[b,f][1,4]diazocin-2(3H) ones (3a-e) have been synthesized. The substituents at fourth position of the phenyl ring for initial and final set of compounds have been selected according to Topliss modified approach. The synthesized compounds were structurally characterized by TLC, elemental analysis, IR and NMR spectra studies. The anticonvulsant potential of synthesized compounds was evaluated by using Rotarod, Actophotometer and Electroconvulsometer. The anticonvulsant activity evaluation of initial set of compounds (3a-d) revealed that electron releasing substituents with high lipophilicity if placed at fourth position in phenyl ring should increase the anticonvulsant activity. Based on this observation, 4-dimethylamino substituted compound (3e) was synthesized and found to have increased activity. Topliss modified approach can be successfully used for the design and development of GABA-nergic anticonvulsants containing dibenzodiazepine skeleton. Top Keywords Dibenzo[1,2,4]triazolo[b,f][1,4]diazocin-2(3H)-one, Topliss approach, Anticonvulsant activity, Gamma amino butyric acid (GABA). Top |