Empirical determination of the degree of analgesic activity of some new 3-aminothieno[2,3-b]pyridines and 1,4-dihydropyridines based on a complex criterion

Authors

DOI:

https://doi.org/10.18413/rrpharmacology.9.10029

Abstract

Introduction: It is revelant to solve the problem of anesthesia based on the research of new highly effective and safe medicines. Among modern studies, the preparation of heterocyclic compounds starting from cyanothioacetamide with analgesic and anti-inflammatory activities is of considerable interest.

Materials and Methods:

The analgesic activity of cyanothioacetamide derivatives was determined on the basis of an integrated approach in three tests: orofacial trigeminal pain, thermal immersion of the tail and in the hot plate test. The experimental characteristics in the studies are quantitative indicators – the frequency of scratching movements n in the first test and the time of the latent period a and t in the second and third tests. Statistical processing consisted in a variance analysis of an array of experimental characteristics. A conditional empirical complex criterion of analgesic activity Anat, inversely proportional to the frequency of scratching movements n and directly proportional to the time of the latent period a and t in the tests is proposed for a comparative assessment of the analgesic activity of the samples.

Results: It is shown that all the studied 1,4-dihydropyridines and condensed thieno[2,3-b]pyridines and reveal analgesic activity of varying degrees of severity, based on the values of the criterion Anat.

Discussion: It was found that the most pronounced analgesic activity was shown by three studied samples: compounds AZ-023, AZ-331 and AZ-383. The complex criterion of analgesic activity of Anat for animals receiving a sample AZ-023 was 50.1, exceeding the indicator in the comparison group by 42 times. The values of this criterion in animals that had received samples AZ-331 and AZ-383 were the highest, namely 64.3 and 68.4, which is 53 and 57 times higher than that of sodium metamizole, respectively.

Conclusion: The obtained results and the advantage of the studied samples over the reference drug determine the expediency of further preclinical studies and a detailed study of their acute and chronic toxicity, as well as hepato-, nephro-, hemato- and gastrotoxicity.

Graphical Abstract

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Keywords:

pain syndrome, analgesic activity, thieno[2,3-b]pyridines, complex criterion

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Author Contribution

Igor V. Bibik, St. Luke Lugansk State Medical University

Candidate of Medical Sciences, Associate Professor of the Department of Surgical Dentistry; e-mail: dr.bibik.i.v@yandex.ru; ORCID ID https://orcid.org/0000-0003-4053-1431. Conducting experiments.

Elena Yu. Bibik, St. Luke Lugansk State Medical University

Doctor Habil. of Medical Sciences, Professor, Head of the Department of Fundamental and Clinical Pharmacology; e-mail: helen_bibik@mail.ru; ORCID ID https://orcid.org/0000-0001-7470-608X. Coordination of research, planning and writing of the manuscript text.

Konstantin A. Frolov, St. Luke Lugansk State Medical University; Vladimir Dahl Lugansk State University

Candidate of Chemical Sciences, Associate Professor of the Department of Pharmaceutical Chemistry and Pharmacognosy, Chief Engineer of the ChemEx Research Laboratory; e-mail: ka.frolov@inbox.ru; ORCID ID https://orcid.org/0000-0002-8045-7582. Synthesis of new compounds.

Sergey G. Krivokolysk, St. Luke Lugansk State Medical University; Vladimir Dahl Lugansk State University

Doctor Habil. of Chemical Sciences, Professor, Senior Researcher, Head of the Department of Pharmaceutical Chemistry and Pharmacognosy, Scientific Director of the ChemEx  Research Laboratory; e-mail: ksg-group-lugansk@mail.ru; ORCID ID https://orcid.org/0000-0001-9879-9217. Synthesis of new compounds, scientific idea and verification of the manuscript.

Victor V. Dotsenko, Kuban State University; North-Caucasus Federal University

Doctor Habil. of Chemical Sciences, Head of the Department of Organic Chemistry and Technology, Leading Researcher of the ChemEx Research laboratory;  e-mail: victor_dotsenko@bigmir.net; ORCID ID  https://orcid.org/0000-0001-7163-0497. Synthesis of new compounds.

Andrey A. Pankov, Vladimir Dahl Lugansk State University

Doctor Habil. of Technical Sciences, Professor of the Department of Transport Technologies; e-mail: app.post@rambler.ru; ORCID ID  https://orcid.org/0000-0003-2813-8231. Theoretical research, scientific idea, statistical data processing and analysis, manuscript design.

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Published

07-06-2023

How to Cite

Bibik IV, Bibik EY, Frolov KA, Krivokolysk SG, Dotsenko VV, Pankov AA (2023) Empirical determination of the degree of analgesic activity of some new 3-aminothieno[2,3-b]pyridines and 1,4-dihydropyridines based on a complex criterion. Research Results in Pharmacology 9(2): 67–74. https://doi.org/10.18413/rrpharmacology.9.10029

Issue

Vol. 9 No. 2 (2023)

Section

Experimental Pharmacology

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