The analgesic activity of new sulfur-containing di- and tetrahydropyridine derivatives in the hot plate test
Abstract
Nowadays the search of new high-efficiency and safe drugs for the pharmacotherapy of diseases accompanied by pain syndrome is an active area of modern pharmacological research.
170 new derivatives of di- and tetrahydropyridines synthesized on the basis of the Chemex Research Laboratory, Vladimir Dahl Lugansk State University were exposed to the virtual bioscreening using the Swiss Target Prediction software. The paper describes screening studies in vivo of 5 samples of sulfur-containing di- and tetrahydropyridines (laboratory codes d02-138, as-262, f02-079, cv-074, cv-143) in the standard hot plate test in comparison with the reference drug — metamizole sodium. The compounds in the dose of 5 mg/kg were given intragastrically 1 hour and a half before placing the rats on the hot plate, the reference drug in the dose of 7 mg/kg also was given intragastrically 1 hour and a half before placing the rats on the hot plate.
The compounds with laboratory codes as-262 (allyl 6-({2-[(4-acetylphenyl)amino]-2-oxoethyl}thio)-5-cyano-4- (2-furyl)-2-methyl-1,4-dihydropyridine-3-carboxylate) and d02-138 (ethyl 4-[({[3-cyano-5-{[(2,4-dichlorophenyl) amino]carbonyl}-4-(2-furyl)-6-methyl-1,4-dihydropyridinе-2-yl]thio}acetyl)amino]benzoate) possess the most pronounced analgesic activity in the dose of 5 mg/kg, they demonstrated 2.03 and 1.9-fold efficiency in comparison to metamizole sodium respectively. The rest three specimens demonstrated metamizole sodium-like analgesic activity.
About the Authors
E. Yu. Bibik
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Bibik Elena Yuryevna — Dr. Sci. (Med.), Professor, Head, Department of Fundamental and Clinical Pharmacology
1g, Kvartal 50-letiya Oborony Luganska, Lugansk, 91045, Lugansk People’s Republic
L. I. Kurbanov
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Kurbanov Latif Ilyasovich — 4th year Student
S. A. Grygoryan
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Grygoryan Stanislav Artashesovich — 4th year Student
D. S. Krivokolysko
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Krivokolysko Dmitryi Sergeevich — Doctoral Student, Department of Fundamental and Clinical Pharmacology
M. A. Kudrina
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Kudrina Marina Andreevna — Postgraduate Student, Department of Pharmaceutical Chemistry and Pharmacognosy
A. A. Pankov
Vladimir Dahl Lugansk State University
Russian Federation
Russian Federation
Pankov Andrey Aleksandrovich — Dr. Sci. (Tech.), Associate Professor, Professor, Department of Transport Technologies
K. A. Frolov
St. Luka Lugansk State Medical University; Vladimir Dahl Lugansk State University
Russian Federation
Russian Federation
Frolov Konstantin Aleksandrovich — Cand. Sci. (Chem.), Associate Professor, Department of Pharmaceutical Chemistry and Pharmacognosy; Chief Engineer, Chemex Scientifi c Lab
V. V. Dotsenko
Vladimir Dahl Lugansk State University; Kuban State University (Krasnodar)
Russian Federation
Russian Federation
Dotsenko Viktor Viktorovich — Dr. Sci. (Chem.), Professor, Department of Organic Chemistry and Technology; Leading Researcher, Chemex Scientific Lab
S. G. Krivokolysko
St. Luka Lugansk State Medical University; Vladimir Dahl Lugansk State University
Russian Federation
Russian Federation
Krivokolysko Sergey Gennadievich — Dr. Sci. (Chem.), Professor, Senior Researcher, Principal Investigator, Chemex Scientific Lab; Head, Department of Pharmaceutical Chemistry and Pharmacognosy
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Review
For citations:
Bibik E.Yu., Kurbanov L.I., Grygoryan S.A., Krivokolysko D.S., Kudrina M.A., Pankov A.A., Frolov K.A., Dotsenko V.V., Krivokolysko S.G. The analgesic activity of new sulfur-containing di- and tetrahydropyridine derivatives in the hot plate test. Journal of Siberian Medical Sciences. 2021;(3):45-55. (In Russ.)
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