| Literature DB >> 25466174 |
Anna Pratima G Nikalje1, Arfat N Shaikh2, Sameer I Shaikh2, Firoz A Kalam Khan2, Jaiprakash N Sangshetti2, Devanand B Shinde3.
Abstract
Herewith, we report the design and synthesis of a series of N-(2-oxo-2((4-oxo-2-substituted thiazolidin-3yl)amino)ethyl) benzamide derivatives 7(a-j) under microwave irradiation, based on four component pharmacophoric model to get structural prerequisite indispensable for anticonvulsant activity. The synthesized derivatives were investigated in maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening. All the test compounds were administered at a dose of 30, 100 and 300 mg/kg body weight at the time interval of 0.5 h and 4 h. The compounds were also evaluated for behavioral activity and toxicity study. The compound 7 h was found to be most active in MES model. The anticonvulsant screening data shows that 65% of the compounds were found active against MES model when compared to 35% sc-PTZ model. The computational parameter such as docking study, logP determination and ADME prediction were performed to exploit the results.Entities:
Keywords: Anticonvulsant evaluation; Benzamide; Computational studies; Microwave irradiation; Thiazolidinone
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Year: 2014 PMID: 25466174 DOI: 10.1016/j.bmcl.2014.11.016
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823