Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry
ISSN: 0975-413X
Sampada S. Jangam
Charak College of Pharmacy and Research, Wagholi, Pune (MS) India -412207, IndiaPublications
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Research Article
Design, Synthesis and Evaluation of Benzothiazole Urea Derivatives as an Anticonvulsant Agent
Author(s): Snehal D. Kachare, Kamalkishor G. Baheti, Qazi Yasar and Sampada S. Jangam
A series of 1-((-6-substituted-2-yl)-3-(4H-1,2,4 triazole-3-yl)urea 7a-f and (1-((3-(6-substituted-2-yl)ureido)methyl)cyclohexyl)acetic acid 8a-fwere designed, synthesized using appropriate synthetic route and screened for CNS depressant and anticonvulsant activities. The synthesized compounds were also analyzed for ADME properties. The results of In-Silico ADME Screening showed that compounds could be exploited as an oral drug candidate. Molecular docking studies were performed for all the synthesized compounds against γ-amino butyric acid amino transferase enzyme (1OHV), All the compounds exhibited docking score in the range of -7.5 to -8.4, among which compound 8c had shown the highest docking scores as compared to the standard drug phenytoin. Animal study for anticonvulsant indicated that compounds 7b, 7e and 8c were exhibited significant activity at a dose 200 mg/kg. All th.. Read More»
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