QSAR Based Design & Synthesis: Design, Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives

Jain, Priyal, Jain, Nilesh, Jain, Vaibhav

ISBN 10: 3846586021 / ISBN 13: 9783846586020

Edité par LAP LAMBERT Academic Publishing, 2012

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N° de réf. du vendeur ERICA79638465860216

Détails bibliographiques

• Titre: QSAR Based Design & Synthesis: Design, Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives
• Éditeur: LAP LAMBERT Academic Publishing
• Date de parution: 2012
• Langue: anglais
• ISBN à 10 chiffres: 3846586021
• ISBN à 13 chiffres: 9783846586020
• Reliure: Paperback
• État de l'article: Like New
• Type de livre: book

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Synopsis

We carried out a QSAR study on benzotriazine derivatives & studied 28 potent GABAA receptor ligands; derivatives of benzotriazines, using a combination of various physicochemical, steric, electronic and thermodynamic descriptors to determine the quantitative correlation between binding affinity and structural features with potent anticonvulsant activity. Correlation between these properties and anticonvulsant activity was used to synthesize compounds possessing potent anticonvulsant activity. Most of the compounds showed an ability to inhibit the maximum electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions. Compound 1A, i.e. 2-(4-Chloro-phenyl)-5-nitro-1H-benzimidazole exhibited maximum activity.