Investigation of antinociceptive properties of new derivatives of 3-aminothieno[2,3-b]pyridine and 1,4-dihydropyridine in the tail immersion test
https://doi.org/10.31549/2542-1174-2023-7-4-23-34
Abstract
I n t r o d u c t i o n . Nowadays, the search for novel painkillers that exhibit both high efficacy and safety profiles is an essential problem of modern pharmacological research.
A i m . To study the antinociceptive activity of ten samples of new derivatives of 3-aminothieno[2,3-b]pyridine and 1,4-dihydropyridine in the classical tail immersion test.
M e t h o d s . 340 new cyanothioacetamide derivatives that were synthesized by us at the Chemex Research Laboratory (Vladimir Dahl Lugansk State University) underwent in silico screening. As a result, 10 compounds were selected that were the most promising for the pharmacological management of pain. In the experiment (tail immersion test), albino male rats were used, divided into 13 groups, 10 animals in each: the intact group, the control group (0.9% sodium chloride solution), the comparison group (metamizole sodium) and 10 experimental groups (according to the number of administered compounds). The compounds were administered intragastrically at a dose of 5 mg/kg 1.5 h before immersing the tail in hot water.
R e s u l t s . It was established that three samples with codenames AZ420, AZ331 and AZ383 showed a significant antinociceptive activity. The tail-flick time of rats in these experimental groups ranged from 31.4 s (AZ331) to 46.4 s (AZ383), while the significance of the differences p in comparison with the values of the control group ranged from 0.00073 (AZ420) to 0.00018 (AZ383).
C o n c l u s i o n s . Four new derivatives of 3-aminothieno[2,3-b]pyridine and 1,4-dihydropyridine with high analgesic activity, promising for further preclinical studies, have been identified.
About the Authors
I. V. Bibik
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Igor V. Bibik – Cand. Sci. (Med.), Assistant, Department of Surgical Dentistry
1G, quarter of the 50th anniversary of the Defence of Lugansk, Lugansk, 91045
K. A. Frolov
St. Luka Lugansk State Medical University; Vladimir Dahl Lugansk State University
Russian Federation
Russian Federation
Konstantin A. Frolov – Cand. Sci. (Chem.), Associate Professor, Department of Pharmaceutical Chemistry and Pharmacognosy; Chief Engineer, Chemex Research Laboratory
Lugansk
V. V. Dotsenko
Vladimir Dahl Lugansk State University; Kuban State University
Russian Federation
Russian Federation
Viktor V. Dotsenko – Dr. Sci. (Chem.), Associate Professor, Head, Department of Organic Chemistry and Technology; Leading Researcher, Chemex Research Laboratory
Krasnodar
Lugansk
S. G. Krivokolysko
St. Luka Lugansk State Medical University; Vladimir Dahl Lugansk State University
Russian Federation
Russian Federation
Sergey G. Krivokolysko – Dr. Sci. (Chem.), Professor, Head, Department of Pharmaceutical Chemistry and Pharmacognosy; Head, Chemex Research Laboratory
Lugansk
E. Yu. Bibik
St. Luka Lugansk State Medical University
Russian Federation
Russian Federation
Elena Yu. Bibik – Dr. Sci. (Med.), Professor, Head, Department of Fundamental and Clinical Pharmacology
Lugansk
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Review
For citations:
Bibik I.V., Frolov K.A., Dotsenko V.V., Krivokolysko S.G., Bibik E.Yu. Investigation of antinociceptive properties of new derivatives of 3-aminothieno[2,3-b]pyridine and 1,4-dihydropyridine in the tail immersion test. Journal of Siberian Medical Sciences. 2023;(4):23-34. (In Russ.) https://doi.org/10.31549/2542-1174-2023-7-4-23-34
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