Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds

Hüseyin İstanbullu; Gülşah Bayraktar; İsmail Öztürk; Güneş Çoban; Merve Saylam

Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds

Abstract

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). 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 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

References

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Details

Primary Language

English

Subjects

Pharmaceutical Chemistry, Pharmaceutical Microbiology

Journal Section

Research Article

Authors

Hüseyin İstanbullu ^*
Türkiye

Gülşah Bayraktar
Türkiye

İsmail Öztürk
Türkiye

Güneş Çoban
Türkiye

Merve Saylam
Türkiye

Publication Date

June 28, 2025

Submission Date

December 18, 2021

Acceptance Date

December 24, 2021

Published in Issue

Year 2022 Volume: 26 Number: 1

IZ

https://izlik.org/JA77RR54SC

Cite

RIS / Bibtex

APA

İstanbullu, H., Bayraktar, G., Öztürk, İ., Çoban, G., & Saylam, M. (2025). Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds. Journal of Research in Pharmacy, 26(1), 231-242. https://izlik.org/JA77RR54SC

AMA

1.İstanbullu H, Bayraktar G, Öztürk İ, Çoban G, Saylam M. Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds. J. Res. Pharm. 2025;26(1):231-242. https://izlik.org/JA77RR54SC

Chicago

İstanbullu, Hüseyin, Gülşah Bayraktar, İsmail Öztürk, Güneş Çoban, and Merve Saylam. 2025. “Design, Synthesis and Bioactivity Studies of Novel Triazolopyrimidinone Compounds”. Journal of Research in Pharmacy 26 (1): 231-42. https://izlik.org/JA77RR54SC.

EndNote

İstanbullu H, Bayraktar G, Öztürk İ, Çoban G, Saylam M (June 1, 2025) Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds. Journal of Research in Pharmacy 26 1 231–242.

IEEE

[1]H. İstanbullu, G. Bayraktar, İ. Öztürk, G. Çoban, and M. Saylam, “Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds”, J. Res. Pharm., vol. 26, no. 1, pp. 231–242, June 2025, [Online]. Available: https://izlik.org/JA77RR54SC

ISNAD

İstanbullu, Hüseyin - Bayraktar, Gülşah - Öztürk, İsmail - Çoban, Güneş - Saylam, Merve. “Design, Synthesis and Bioactivity Studies of Novel Triazolopyrimidinone Compounds”. Journal of Research in Pharmacy 26/1 (June 1, 2025): 231-242. https://izlik.org/JA77RR54SC.

JAMA

1.İstanbullu H, Bayraktar G, Öztürk İ, Çoban G, Saylam M. Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds. J. Res. Pharm. 2025;26:231–242.

MLA

İstanbullu, Hüseyin, et al. “Design, Synthesis and Bioactivity Studies of Novel Triazolopyrimidinone Compounds”. Journal of Research in Pharmacy, vol. 26, no. 1, June 2025, pp. 231-42, https://izlik.org/JA77RR54SC.

Vancouver

1.Hüseyin İstanbullu, Gülşah Bayraktar, İsmail Öztürk, Güneş Çoban, Merve Saylam. Design, synthesis and bioactivity studies of novel triazolopyrimidinone compounds. J. Res. Pharm. [Internet]. 2025 Jun. 1;26(1):231-42. Available from: https://izlik.org/JA77RR54SC