Facile Synthesis of N-(4-Bromo-3-methylphenyl)pyrazine-2-carboxamide Derivatives, Their Antibacterial Activities against Clinically Isolated XDR S. Typhi, Alkaline Phosphatase Inhibitor Activities, and Docking Studies DOI Creative Commons

Abdul Hannan Khan,

Muhammad Bılal, Abid Mahmood

et al.

Pharmaceuticals, Journal Year: 2024, Volume and Issue: 17(9), P. 1241 - 1241

Published: Sept. 20, 2024

The emergence of extensively drug-resistant Salmonella Typhi (XDR-S. Typhi) poses a grave public health threat due to its resistance fluoroquinolones and third-generation cephalosporins. This significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (3, 5a–5d) in good yields through Suzuki reaction. Afterward, evaluate their antibacterial activities against XDR-S. via agar well diffusion method; 5d has strongest activity with MIC 6.25 (mg/mL). Moreover, vitro Alkaline Phosphatase inhibitor was also determined; is most potent compound, an IC50 1.469 ± 0.02 µM. Further, silico studies were performed find type interactions between compounds target proteins.

Language: Английский

Facile Synthesis of N-(4-Bromo-3-methylphenyl)pyrazine-2-carboxamide Derivatives, Their Antibacterial Activities against Clinically Isolated XDR S. Typhi, Alkaline Phosphatase Inhibitor Activities, and Docking Studies DOI Creative Commons

Abdul Hannan Khan,

Muhammad Bılal, Abid Mahmood

et al.

Pharmaceuticals, Journal Year: 2024, Volume and Issue: 17(9), P. 1241 - 1241

Published: Sept. 20, 2024

The emergence of extensively drug-resistant Salmonella Typhi (XDR-S. Typhi) poses a grave public health threat due to its resistance fluoroquinolones and third-generation cephalosporins. This significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (3, 5a–5d) in good yields through Suzuki reaction. Afterward, evaluate their antibacterial activities against XDR-S. via agar well diffusion method; 5d has strongest activity with MIC 6.25 (mg/mL). Moreover, vitro Alkaline Phosphatase inhibitor was also determined; is most potent compound, an IC50 1.469 ± 0.02 µM. Further, silico studies were performed find type interactions between compounds target proteins.

Language: Английский

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