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Antibacterial and Acetylcholinesterase Inhibitory Potentials of Triazenes Containg Sulfonamide Moiety

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Pharmaceutical Chemistry Journal Aims and scope

The aim of this study was to investigate the antibacterial and acetylcholinesterase (AChE) inhibitory activities of 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl)benzenesulfonamides (compounds 1 – 12) and to find out new possible drug candidate molecules since the available agents in clinical use have some limitations. According to the results of antibacterial screening for compounds 1 – 12, most of the synthesized compounds were found to be effective against Gram-positive microorganisms while being ineffective (MIC > 1600 μg/mL) on Gram-negative microorganisms. According to the AChE inhibition results, Ki values of compounds 1 – 12 were in the range of 5 ± 1 – 34 ± 2 nMtoward AChE. Tacrine (TAC) used as a reference drug had Ki value of 4 ± 1 nM toward AChE. The non-substituted derivative compound 1 coluld be considered as a lead compound for this study in terms of AChE inhibitory activity, since its Ki value (5 ± 1 nM) was close to that of the reference drug (TAC). Thus, compound 1 was docked at the binding site of AChE and showed good interaction with the target enzyme, suggesting their possible mechanism of action.

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ACKNOWLEDGMENTS

The authors thank Ruya Kaya (Ibrahim Cecen University, Turkey) for her contributions to the AChE inhibition assay.

CONFLICT OF INTEREST

The authors declare no conflict of interest.

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Authors and Affiliations

  1. Ataturk University, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, TR-25240, Erzurum, Turkey

    Sinan Bilginer & Halise Inci Gul

  2. Ataturk University, Department of Pharmaceutical Microbiology, Faculty of Pharmacy, TR-25240, Erzurum, Turkey

    Hayrunisa Hanci

  3. Ataturk University, Department of Chemistry, Faculty of Science, Erzurum, Turkey

    Ilhami Gulcin

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  1. Sinan Bilginer
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  2. Halise Inci Gul
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Correspondence to Sinan Bilginer.

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Bilginer, S., Gul, H.I., Hanci, H. et al. Antibacterial and Acetylcholinesterase Inhibitory Potentials of Triazenes Containg Sulfonamide Moiety. Pharm Chem J 55, 284–289 (2021). https://doi.org/10.1007/s11094-021-02412-1

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  • DOI: https://doi.org/10.1007/s11094-021-02412-1

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