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
1 - Tver State Medical University, Tver, Russia
2 - State 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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