A series of new 2-(4/3-substitutedbenzyl)thieno[2,3-d]pyrimidin-4(3H)-ones (2a-f) and 2-(4/3-substituted benzyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one derivatives (3a-f) were synthesized for the first time by the reaction of corresponding 2-aminothiophene-3-carboxamide derivatives and appropriate iminoester hydrochlorides under suitable conditions. Using microdilution method, the antibacterial and antifungal activities of the synthesized compounds were tested against selected strains of Gram positive and Gram negative bacteria (Staphylococcus aureus, Enterecoccus faecalis, Escherichia coli and Pseudomonas aeruginosa) and yeast-like fungi (Candida albicans, C. krusei and C. parapsilosis). In these tests, compounds 3a-f showed higher antifungal activity than fluconazole against Candida fungus species. 2-Substituted thieno-[2,3-d]pyrimidin-4(3H)-ones (2a-f) showed better antibacterial activity than 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one derivatives (3a-f).
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Acknowledgements
This study was supported by the Scientific Research Project Coordination Unit of Karadeniz Technical University. Project number: FBA-2016-5461.
We would like to thank Assist. Prof. Dr. Hasan SAĞLAMEL for the English review. We would like to thank Statistician Tuðba GÜVEN
KURT, KTÜ Farabi Hospital, Statistical Unit for the statistical data analysis.
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Kahveci, B., Doğan, İ.S., Menteşe, E. et al. Synthesis and Antibacterial and Antifungal Activity of New Thieno[2,3-d]Pyrimidin-4(3H)-One Derivatives. Pharm Chem J 54, 647–653 (2020). https://doi.org/10.1007/s11094-020-02252-5
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DOI: https://doi.org/10.1007/s11094-020-02252-5