Prediction and Study of Anticonvulsant Properties of Benzimidazole Derivatives

Anticonvulsive activities of some condensed imidazo[1,2- a ]benzimidazole derivatives were predicted using PASS software. Benzimidazoles as a class showed promise as sources of anticonvulsants. Several compounds demonstrated various levels of anticonvulsive activity in the corazole-induced seizure m...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2017-03, Vol.50 (12), p.775-780
Main Authors: Vasil’ev, P. M., Kalitin, K. Yu, Spasov, A. A., Grechko, O. Yu, Poroikov, V. V., Filimonov, D. A., Anisimova, V. A.
Format: Article
Language:English
Subjects:
Analysis
Divalproex
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Ruthenium
Search for New Drugs
Seizures (Medicine)
Valproic acid
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Summary:Anticonvulsive activities of some condensed imidazo[1,2- a ]benzimidazole derivatives were predicted using PASS software. Benzimidazoles as a class showed promise as sources of anticonvulsants. Several compounds demonstrated various levels of anticonvulsive activity in the corazole-induced seizure model (75 mg/kg, s.c.). The most promising compounds (laboratory codes RU-1205, RU-285, RU-1204, and RU-1203) at a dose of 10 mg/kg (i.p.) showed high levels of anticonvulsive activity comparable with that of reference valproic acid (130 mg/kg, i.p.) at a molar ratio of ~1:30. The Free—Wilson model was used to describe quantitative structure—activity relationships in order to evaluate contributions of substituents or structural fragments to the anticonvulsive activity of the parent structure. Four pharmacophore patterns that favored high anticonvulsive activity among imidazo[1, 2- a ]benzimidazole derivatives were found using IT Microcosm.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-017-1530-6