Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2022 , Vol 26 , Issue 1
Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Izmir Katip Celebi University, Izmir, Turkey
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Izmir, Turkey
3Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Izmir Katip Celebi University, Izmir, Turkey
DOI : 10.29228/jrp.121 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 (Candida albicans and Candida parapsilosis). Anti-biofilm 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 μg/ml dose against E. coli and P. aeruginosa and a decreasing effect on the relative accumulation of ethidium bromide in P. aeruginosa at 100 μg/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. Keywords : Antimicrobial resistance; triazolopyrimidinone; N-(methylnaphthalene)piperazine; microwave-assisted synthesis; ethidium bromide accumulation; anti-biofilm activity
Marmara University