Authors
Malygin A. S.
Post-graduate student, Chair for Pharmacology and Clinical Pharmacology1
Yasnetsov V. V.
Doctor of Medicine, Leading Researcher, Chair for Experimental and Clinical Pharmacology2
1Tver State Medical University, Tver, Russia
2State Scientific Center of the Russian Federation – Institute of Medical and Biological Problems of the Russian Academy of Sciences, Moscow, Russia
Corresponding author
Malygin A.S.; e-mail: dr.a.s.m@yandex.ru
Conflict of interest
None declared.
Funding
The study had no sponsorship.
Abstract
Pharmacophoric analysis of the structure of valprazolamide, a 1,3,4-thiadiazolylamide derivative of valproic acid, was carried out. It was shown that the new valproate contains a substituted amide group, hydrophobic and electron-donor domåns – pharmacophores, determining its antiepileptic activity. Valproic acid has only a hydrophobic moiety. Modification of valproic acid by introducing an additional pharmacophore, 1,3,4-thiadiazole, into its structure leads to a decrease in toxicity and an increase in antiepileptic activity.
Key words
pharmacophoric analysis, valproic acid, 1,3,4-thiadiazole, antiepileptic activity
DOI
References
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