Studying of analgesic and anti-inflammatory activity of 2,4-dioxobutanoic acid hydrazine derivatives

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Abstract

Objective. To study the analgesic and anti-inflammatory activity of water-soluble hydrazine derivatives of 2,4-dioxobutanoic acids, as well as to determine the relationship between the structure of substances and their biological effects.

Materials and methods. The laboratory synthesis methods were applied to obtain 2-hydrazine derivatives of 2,4-dioxobutanoic acids. The compounds were tested for biological activity using a hot plate test in mice and an acute inflammatory reaction caused by carrageenan-induced paw edema in rats.

Results. The analgesic activity of four compounds is comparable to that of nimesulide. One of the substances obtained is found to exhibit higher anti-inflammatory activity than nimesulide during the 1st and 3rd hours of the experiment. Two compounds with a combination of high analgesic and anti-inflammatory activity were identified. The effect of certain radicals in the structure of the substances on the activities studied was discovered.

Conclusions. The revealed relationship between the structure of original compounds and their biological activities can be used in the further synthesis and search for new domestic pharmaceutical substances with investigated effects.

About the authors

Natalia A. Pulina

Perm State Pharmaceutical Academy

Email: pulina-nata@mail.ru

Doctor of Pharmaceutical Sciences, Professor, Head of Department of Pharmaceutical Technology

Russian Federation, Polevaya st. 2, Perm, 614990

Aleksander S. Kuznecov

Perm State Pharmaceutical Academy

Author for correspondence.
Email: alexanderiv.88@mail.ru

Candidate of Pharmaceutical Sciences, Associate Professor, Department of General and Organic Chemistry

Russian Federation, Polevaya st. 2, Perm, 614990

Svetlana V. Chashchina

Perm State Pharmaceutical Academy

Email: physiology@list.ru

Candidate of Biological Sciences, Associate Professor, Department of Physiology

Russian Federation, Polevaya st. 2, Perm, 614990

References

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  5. Pulina N.A., Kozhukhar V.Yu., Kuznetsov A.S., Starkova A.V., Rubtsov A.E. Synthesis and search for compounds with hemostatic activity in the series of 4-(het)aryl-4-oxobut-2-enoic acid derivatives. Russian Chemical Bulletin 2017; 8: 1497–1502 (in Russian).
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Copyright (c) 2020 Pulina N.A., Kuznecov A.S., Chashchina S.V.

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