The analgesic activity research for the derivatives of 4-R-3-(morpholinomethylene)-1,2,4-triazole-5-thioles
Journal Title: Фармацевтичний журнал - Year 2014, Vol 6, Issue 6
Abstract
Pain is a protective reaction of the organism, which is the first sign of illness or signal of danger. Existing drugs for pain reducing exhibits a series of side effects. However, with an analgesic effect, most of these preparations displays lot of side effects. Thus, the searching for new highly effective and safe drug with pronounced analgesic activity is an actual problem of modern medicine and pharmacy. The purpose of our studies was to investigate the analgesic properties of some derivatives of 4-R-3-(morpholinomethylene)-1,2,4-triazole-5-thioles and detection of some regularities according to pharmacological activity and the chemical structure of synthesized compounds. For studying the analgesic effect of new derivatives of 1,2,4-triazole, and determine the effect of the central component in the nociceptive system the model of thermal limbs stimulation («hot plate») was used. The study has found of that most from tested compounds under the experimental conditions reduced the pain threshold in laboratory animals. However, the replacement of methyl substituent at N1 atom of nitrogen in molecule 3-(morpholinomethylene)-4-methyl-1,2,4-triazole-5-thiol (PKR-125) for phenyl substituent (PKR-123) leads to a slight analgesic activity. It has been established, that the appearance of carboxylic group in the molecule reduces the analgesic effect of some synthesized compounds.
Authors and Affiliations
E. V. Kapelyanovich, R. О. Shcherbyna, E. S. Pruglo, О. І. Panasenko, Ye. G. Knysh
Keywords
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