MICROWAVE ASSISTED SYNTHESIS AND EVALUATION OF ANTICONVULSANT ACTIVITY OF SOME 1, 4-DIHYDROPYRIDINE DERIVATIVESAbstract
In the view of an extensive literature survey that revealed the anticonvulsant profile of 1,4-dihydropyridines and 1,3,4-Thiadiazole, we have coupled these two moieties with the aim of achieving an enhanced anticonvulsant effect. In present investigation some of ethyl-1-((5-amino-1, 3, 4-thiadiazol-2-yl) methyl)-5-ethyl-2, 6-dimethyl-4-substituted phenyl-1, 4-dihydro-pyridine-3-carboxylate derivatives are synthesized through four steps. A greener approach is employed by using Chloramine-T as an efficient and safer oxidative catalyst for the synthesis of Thiadiazole and the use of the Microwave technique for accelerating the chemical reactions. The structures of the newly synthesized compounds were confirmed on the basis of IR, 1H-NMR, and Mass analyses. An acute toxicity study was done to determine LD50 of the newly synthesized compounds. Some of the synthesized compounds were evaluated for their anticonvulsant effect by PTZ induced convulsions method. Statistical testing was done by one-way ANOVA followed by Dunnett’s test. The compounds F123 and showed the highest percentage of protection against convulsions at the dose of 15 mg/kg among the evaluated compounds compared to control.
D. D. Rishipathak * and K. V. Patil
Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, (Savitribai Phule Pune University, Pune), Adgaon, Nashik, Maharashtra, India.
03 April 2020
28 October 2020
15 March 2021
01 April 2021