Anticonvulsant activity of 5-(furan-2-yl)-4R1-1,2,4-triazole-3-thione S-derivatives
Abstract
Among the huge number of drugs registered in Ukraine anticonvulsants occupy a special place. They are mainly used for the relief of different etiology seizures. Along with the principal pharmacological action of drugs in this group there were exhibited a number of unwanted side effects. Therefore the question of the searching for new biologically active molecules, remains relevant today and is necessary for the further practical introduction into medical practice.
The purpose of our work was to study the anticonvulsant activity of 5- (furan-2-yl) -4R1-1,2,4-triazole-3-thione S-derivatives.
The anticonvulsant activity study of the 5-(furan-2-yl)-2H-1,2,4-triazole-3-thione S-derivatives and 5-(furan-2-yl)-4-phenyl-4H-1,2,4-triazole-3-thiones were conducted on the test of interaction with agents that stimulate the central nervous system. The theoretical computer predictions indicate the prospects in searching among the represented compounds classes. The criteria for assessing anticonvulsant activity were the changings in attack seizures latency and their duration. Reference drugs were Mydocalmum and Phenobarbital. Among the studied substances two compounds had the highest activity which is equivalent in strength to the activity of reference drugs.
Two compounds among the studied substances have the highest activity which is equivalent in strength to Mydocalm activity/ Also 2-[5-(furan-2-yl)-4-fenil-4H-1,2,4-triazole-3-ylthio]-1-(4-chlorfeniletanon) must be noted, whose activity exceeds the activity of Phenobarbitalum and Midokalm in 1,23 and 1,27 times respectively on korazol model of seizures in rats. For some classes of 1,2,4-triaxole-3-thione 5-furanderivatives there were established structure–action patterns.
References
2. Bilay I. M., Galushko A. Yu., Gnyko IV V. et al. Hypolipidemic activity of some derivatives of 1,2,4-triazole // Act. question of pharmacy. honey. science and practice. - 2013. - No. 1 (11). - P. 15-17.
3. Parkhomenko L. I., Al Nuri Ahmed, Ershov N. A. and others. Influence of triazolin derivatives on incubation, morphological parameters of blood and productivity of broiler chickens / Sat. scientific works "Modern problems and ways of their solution in science, transport, production and education - 2013". - Odessa, 2013. - Vol. 46. - P. 47-53.
4. Bilay I. M., Mikhailyuk E. O., Parchenko V. V. and others. Medium-effective dose of 4-amino-5- (furan-2-yl) -4H-1,2,4-triazole-3-thiol in experimental hepatitis // Zaporozhye. honey. journ - 2014 - No. 2 (83). - P. 100-102.
5. Parchenko V.V. Synthesis, transformation, physical-chemical and biological properties in a number of 5-furyl-substituted 1,2,4-triazole-3-thione. Dis ... Dr. farm. sciences - Zaporozhye, 2014. - 361 p.
6. Parchenko V.V. Synthesis, physico-chemical and biological properties of derivatives of 1,2,4-triazole-3-thione containing the core of furan. Dis ... Candidate farm sciences - Kyiv, 2006. - 207 p.
7. Gotsulya AS, Kaplushenko A.G., Parchenko V.V. and others. Computer forecasting of possible types of biological activity of S-derivatives of 1,2,4-triazole // Zaporozhye. honey. journ - 2008. - No. 1. - P. 122-124. 7
8. Pre-clinical study of the specific activity of potential anti-convulsant drugs. Method. Recommendations / Ed. acad. M.Ya. Golovenko, prof. L. O. Gromova. - K., State Pharmacological Center MoH Ukraine, 2003. - 46 p.
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