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.
Highlights
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
Analysis of the cultured collection strains P. mirabilis showed that the compounds codified as PYaTs3 and PYaTs4 suppress their growth within the concentration range of 128-4 μg/ml, with a concentration of 8-4 μg/ ml being the MIC50 and 128 μg/ml corresponding to the MIC85–MIC100, i.е. close to bactericidal
These strains displayed sensitivity for the PYaTs2 compound in, but within, the concentration ranges of 128-16 μg/ml: the MPC50 corresponded in most cases to 32 μg/ml and, with 128 μg/ml, the growth rate decreased by 65–6% at the most
Summary
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. 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. Conclusion: 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. Urinary tract infections are amongst the most common bacterial infections in humans caused by bacteria of the genus Proteus (P. vulgaris, P. mirabilis, P. rettgeri) (Pellegrino et al 2013, Budnik 2015, Liu et al 2015). There is an increased interest towards the role of Proteus in the etiology of rheumatoid arthritis (RA) and towards the development of chemotherapeutic drugs which are active against protei that can reduce the risk of and/or worsening RA development (Ushakova et al 2001, Disaanayake et al 2014)
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
