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BIOLOGICAL ACTIVITY OF NEW DERIVATIVES OF TRIAZOLES

DOI: https://doi.org/None
Issue: 
3
Year: 
2017

L.N. Ovsyannikova; B.Yu. Lalaev, PhD; Professor I.P. Yakovlev, PhD; N.A. Anisimova, PhD; E.N. Kirillova, PhD; G.V. Ksenofontova, PhD Saint Petersburg State Chemopharmaceutical Academy; 14, Prof. Popov St., Saint Petersburg 197376, Russian Federation

Introduction. A study of previously obtained 1,3-oxazines has shown that they have anti-inflammatory, sedative, and antimicrobial activities. The biological activity of the products of their interaction with nitrogen-containing binucleophilic reagents has not been studied. Objective: to investigate the biological activity of new synthesized 1,2,4-triazole derivatives. Material and methods. The probable types of biological activity were predicted using the PASS software. Experiments on outbred male albino mice determined the acute toxicity of 1,2,4-triazole derivatives. Antifungal activity was established from the lowest inhibitory concentration of the test compounds. Antimicrobial effect was determined by the absence of growth of the test microorganisms in the meat-peptone broth containing the lowest concentration of a drug, and the nature of antimicrobial (bacteriostatic or bactericidal) activity was ascertained in the absence of their growth in a nutrient dense medium. Anti-inflammatory activity was investigated using an acute formalin-induced paw swelling in rats. Analgesic activity was established by applying an acetic acid-induced writhing model in mice. Results. 1,2,4-triazoles were referred to as a class of non-toxic substances (LD50, 1250 to 2000 mg/kg). These were inferior to comparison drugs in antifungal and antibacterial activities. The anti-inflammatory effect of 1,2,4-triazoles was slightly below that of the comparison drug, but the former had a very low toxicity. The analgesic activity of the test compounds was higher than that of the comparison drug. Conclusion. The new synthesized 1,2,4-triazole derivatives are non-toxic and possess pronounced anti-inflammatory and analgesic activities.

Keywords: 
1
2
4-triazoles
biological activity
PASS software
acute toxicity
antifungal
antimicrobial
anti-inflammatory
and analgesic activities

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