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Synthesis and Antibacterial Activity of Novel 3-N-Substituted 1,8-Naphthyridin-2(1H)-ones

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Abstract

Synthesis of novel N-protected and unprotected 3-N-substituted 1,8-naphthyridin-2(1H)-ones with potential inhibiting activity of penicillin-binding protein 6 (PBP6) has been developed. The synthesis is designed around a Buchwald–Hartwig crosscoupling of various 3-bromo-6-substituted-1,8-naphthyridin-2(1H)-ones with two different functionalized anilines. According to the preliminary antibacterial evaluation, the products 9b9d and 10b10d have demonstrated high inhibiting activity against spore germination of Staphylococcus aureus (gram positive) and Escherichia coli (gram negative). The molecular docking procedure has denoted the probable interactions of the synthesized compounds 9b9d and 10b10d with the target protein.

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Funding

One of the Kurumanna A authors would like to thank UGC for research leading to these results has received from SRFfellowship providing for us, and also thank CFRD-OU for analytical support.

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Correspondence to B. Sakram.

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Sakram, B., Kurumanna, A., Ashok, K. et al. Synthesis and Antibacterial Activity of Novel 3-N-Substituted 1,8-Naphthyridin-2(1H)-ones. Russ J Gen Chem 89, 2534–2543 (2019). https://doi.org/10.1134/S1070363219120338

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  • DOI: https://doi.org/10.1134/S1070363219120338

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