Investigation of the activity of new derivatives of 1,3-diazinone-4 and their acyclic precursors with respect to bacteria of the genus Proteus

Abstract

Introduction: The present paper provides a study of the activity of the new 1,3-diazinon-4 derivatives and their acyclic precursors under the laboratory cipher PYaTd1, PYaTs2, PYaTs3 and PYaTs4 against microorganisms of the genus Proteus, which is of high importance at the moment as the growing resistance of the Proteus to previously highly active antibiotics dictates the need to search for effective antimicrobial agents that meet modern safety requirements.

Materials and Methods: The study of the activity of the compounds was carried out on collection and freshly isolated strains from patients with different pathologies. The strains were identified using the BIOMIC V3 apparatus (Giles Scientific, USA) to verify genus and species identity. The strains used in the study were previously examined for sus­ceptibility to antibacterial drugs by the Disc Method to assess the presence or absence of resistance. The activity of the new compounds was studied by the serial dilution method.

Results: The results of the study showed that the compounds PYaTd1, PYaTs2, PYaTs3 and PYaTs4 show a different activity against bacteria of the genus Proteus. The substance PYaTs2 is ineffective. With respect to strains P. mirabilis and P. rettgeri, the minimum inhibitory concentration of the compounds PYaTs3, PYaTs4 and PYaTd1 ranges from 4 μg/ml to 16 μg/ml.

Conclusion: Thus, by the average aggregate indices, regardless of the species and strain of bacteria, the most effective compound is PYaTd1, the MIC₅₀ of which is within 10 μg/ml, which proves it to be promising and makes further de­velopment worthwhile.