Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds

Autor:	Huseyin Istanbullu, Gulsah Bayraktar, Ismail Ozturk, Gunes Coban, Merve Saylam
Jazyk:	angličtina
Rok vydání:	2022
Předmět:	triazolopyrimidinone ethidium bromide accumulation anti-biofilm activity Antibiotics Antimicrobial Drug Susceptibility Efflux Pump Inhibitor 1-(1-Naphthylmethyl)-Piperazine N-(methylnaphthalene)piperazine Biological Evaluation Agents Antimicrobial resistance microwave-assisted synthesis Series
Popis:	This study was aimed to develop novel compounds to combat antimicrobial resistance, which is one of the biggest threats to global health. For this purpose, compounds bearing triazolopyrimidinone ring and N-(methylnaphthalene)piperazine (NMP) hybrids were designed and synthesized. Ten new compounds were synthesized and after proving their chemical structures were tested for antimicrobial activity using disk diffusion and microdilution method against Gram-negative bacterial strains (Escherichia coli and Pseudomonas aeruginosa), Gram-positive bacterial strains (Staphylococcus aureus and Enterococcus faecalis) and fungal strains (Candid(' albicans and Candida parapsilosis). Antibiofilm activity and ethidium bromide accumulation assay results were also determined for the selected compounds. Among the tested compounds, hybrid compound H5 showed promising activity against E. faecalis with 16-fold potency compared to its precursor, TP5. Additionally, it has statistically significant inhibition of biofilm production at 10 mu g/ml dose against E. coli and P. aeruginosa and a decreasing effect on the relative accumulation of ethidium bromide in P. aeruginosa at 100 mu g/ml dose (85.07%) after 30 min. 2,5-disubstitued[1,2,4]triazolo[1,5-a]pyrimidinone heterocyclic core structure and its antimicrobial activity are reported to the literature for the first time in this study. Izmir Katip Celebi University [2018-ONAP-ECZF-0003, 2018-ONAP-ECZF-007] This study was supported by research grants from Izmir Katip Celebi University (Project number 2018-ONAP-ECZF-0003 and 2018-ONAP-ECZF-007. The authors gratefully acknowledge Pharmaceutical Sciences Research Center (FABAL) of the Faculty of Pharmacy, Ege University for providing spectral analysis.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8f5b4ef8c4a2c117706a23f9e51d64a https://hdl.handle.net/11454/78354 Zobrazit plný text záznamu