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BIOLOGICAL ACTIVITY OF HYDROGENALIDES OF AMIDEZONE

Abstract

The biological activity of a number of N'-arylbenzenecarbоximidohydrazide hydrohalides in vitro against Staphylococcus aureus, Bacillus cereus, Escherichia coli and Candida albicans and Aspergillus brasiliensis fungi, as well as anti-inflammatory and analgesic activities in vivo has been studied. N'-(4-nitrophenyl)benzenecarboximidohydrazide hydrochloride (3c) exhibits marked antimicrobial activity against St. aureus, 4-nitro-N'-phenylbenzenecarboximidohydrazide hydrochloride (3b) is effective against C. albicans and A. brasiliensis fungi. Acute toxicity of the obtained compounds for mice with intragastric administration was 1000 to 2000 mg/kg and intraperitoneal administration was 200 to 400 mg/kg. 4-nitro-N'-phenylbenzenecarboximidohydrazide hydrochloride (3b) has anti-inflammatory and analgesic activities that do not exceed that of the reference preparations.

About the Authors

A. S. Senina
St. Petersburg Chemical and Pharmaceutical Academy
Russian Federation


A. V. Moskvin
St. Petersburg Chemical and Pharmaceutical Academy
Russian Federation


S. V. Gurina
St. Petersburg Chemical and Pharmaceutical Academy
Russian Federation


E. L. Avinirova
St. Petersburg Chemical and Pharmaceutical Academy
Russian Federation


References

1. Всемирная организация здравоохранения. URL: http://www.who.int/ru/ (дата обращения 20.11.2017).

2. Б.В. Пассет. Технология химико-фармацевтических препаратов и антибиотиков. - М.: Медицина, 1977.

3. D.G. Neilson. Chemistry Departament. - Scotland. 1969. P. 151-170.

4. PASS. URL: http://www.way2drug.com/PASSOnline/info.php (дата обращения 20.11.2017).

5. А.А. Евдокимов, А.С. Сенина, А.В. Москвин, И.А. Фридман, И.П. Яковлев, С.В. Гурина. Синтез, строение и биологическая активность некоторых амидразонов // Бутлеровские сообщения. 2014. Т. 39. № 8. С. 87-90.

6. D.A. Filimonov, V.V. Poroikov. Chemoinformatics Approaches to Virtual Screening / Ed. by A. Varnek and A. Tropsha. - Cambridge (UK): RSC Publishing, 2008. P. 182-216.

7. ChEMBLdb // The European Bioinformatics Institute Part of the European Molecular Biology Laboratory [Official website]. URL: https://www.ebi.ac.uk/chembldb/ (дата обращения 04.03.2013).

8. П.В. Погодин, А.А. Лагунин, С.М. Иванов, В.И. Конова, Д.А. Филимонов, В.В. Поройков. Компьютерный прогноз взаимодействия низкомолекулярных органических соединений с белками-мишенями // Вестник РГМУ. 2013. № 4. C. 69-74.

9. Государственная фармакопея Российской Федерации. XIII изд. Т. 1. - М. 2015. C. 848-923.

10. Руководство по проведению доклинических исследований лекарственных средств. Ч. 1. - М.: Гриф и К, 2012. 944 с.

11. A.S. Senina, A.A. Evdokimov, A.V. Moskvin, E.V. Fedorova. Synthesis, Characterization and Antimicrobial Activity of Amidrazone Derivatives // Journal of Advanced Chemical Sciences. V. 2. Is. 1. 2016. Р. 183-187.

12. H.U. Zeilhofer, D. Benke, G.E. Yevenes. Chronic pain states: pharmacological strategies to restore diminished inhibitory spinal pain control // Annu. Rev. Pharmacol. Toxicol. 2012. V. 52. Р. 111-133.


Review

For citations:


Senina A.S., Moskvin A.V., Gurina S.V., Avinirova E.L. BIOLOGICAL ACTIVITY OF HYDROGENALIDES OF AMIDEZONE. Drug development & registration. 2018;(1):180-185. (In Russ.)

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ISSN 2305-2066 (Print)
ISSN 2658-5049 (Online)