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ANTIMICROBIAL ACTIVITY OF AMIDRAZONE HYDROHALOGENIDES

DOI: https://doi.org/None
Issue: 
8
Year: 
2017

A.S. Senina; S.V. Gurina, PhD; Professor A.V. Moskvin, PhD Saint Petersburg State Chemopharmaceutical Academy; 14, Prof. Popov St., Saint Petersburg 197376, Russian Federation

Introduction. There is now an increase in the resistance of many pathogens to commonly used antimicrobial drugs. The representatives of a class of amidrazones exhibit antibacterial and antiviral activities. They are available, highly reactive, and good intermediates in the synthesis of other compounds possessing a wide spectrum of biological activity. Objective: to determine the antimicrobial activity of the synthesized derivatives of amidrazone and the most active compounds. Material and methods. The object of the investigation was synthesized amidrazone derivatives. The obtained compounds were ascertained to have in vitro antimicrobial activity against the test cultures of Staphylococcus aureus, Bacillus cereus, and Escherichia coli and the fungi Candida albicans and Aspergillus brasiliensis. The investigations were conducted in accordance with the procedures described in the State Pharmacopoeia of the Russian Federation XIII edition. Results. Amidrazones were established to be bound to the selected protein targets more effectively than the known antimicrobial agents. All the test compounds were virtually inactive against the cultured bacteria E. coli and Bac. cereus. The antimicrobial activity of amidrazones against St. aureus depended on the nature of a substituent inserted into the molecule. The greatest activity was shown by the compounds containing the nitro group at the para-position of a phenylhydrazine moiety. The compounds having pronounced antifungal properties against C. аlbicans were identified. Conclusion. Hydrohalogenides of the synthesized amidrazones have antimicrobial activity against St. aureus, C. аlbicans, and A. brasiliensis. The antimicrobial activity of the compounds has been shown to depend on the electronic nature of substituents in the aryl moieties of the amidrazone molecule. The most promising compounds which have a pronounced antistaphylococcal and antifungal activities have been identified.

Keywords: 
amidrazone hydrohalogenides
antimicrobial activity
fungicidal activity

References: 
  1. Vsemirnaya organizaciya zdravoohraneniya. [E`lektronnyy resurs]. Rezhim dostupa: http://www.who.int/ru/
  2. Passet B.V. Tehnologiya himiko-farmacevticheskih preparatov i antibiotikov. M.: Medicina, 1977.
  3. Neilson D.G. Chemistry Department, The University, Dundee, Angus, R. Roger. Scotland, 1969; 151–70.
  4. Evdokimov A.A., Senina A.S., Moskvin A.V. i dr. Sintez, stroenie i biologicheskaya aktivnost` nekotoryh amidrazonov. Butlerovskie soobshheniya, 2014; 39 (8): 87–90.
  5. Filimonov D.A., Poroikov V.V. Chemoin for matics Approaches to Virtual Screening (ed. by A.Varnek, A.Tropsha) Cambridge (UK): RSC Publishing, 2008; 182–216.
  6. ChEMBLdb. The European Bioinformatics Institute Part of the European Molecular Biology Laboratory [Electronic resource. Official website]. URL: https:// www.ebi.ac.uk/chembldb/
  7. Pogodin P.V., Lagunin A.A., Ivanov S.M. i dr. Komp`yuternyy prognoz vzaimodeystviya nizkomolekulyarnyh organicheskih soedineniy s belkami-mishenyami. Vestnik RGMU, 2013; 4: 69–74.
  8. Gosudarstvennaya farmakopeya RF XIII izd., tom 1. M., 2015; 848–923.
  9. Senina A.S., Evdokimov A.A., Moskvin A.V., Fedorova E.V. Synthesis, Characterization and Antimicrobial Activity of Amidrazone Derivatives. Journal of Advanced Chemical Sciences, 2016; 2 (1): 183–7.