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

Autor: Abdul Hannan Khan, Muhammad Bilal, Abid Mahmood, Nasir Rasool, Muhammad Usman Qamar, Muhammad Imran, Sebastian Ionut Toma, Oana Andreescu
Jazyk: angličtina
Rok vydání: 2024
Předmět:
Zdroj: Pharmaceuticals, Vol 17, Iss 9, p 1241 (2024)
Druh dokumentu: article
ISSN: 17091241
1424-8247
23491582
DOI: 10.3390/ph17091241
Popis: The emergence of extensively drug-resistant Salmonella Typhi (XDR-S. Typhi) poses a grave public health threat due to its resistance to fluoroquinolones and third-generation cephalosporins. This resistance 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 the Suzuki reaction. Afterward, we evaluate their antibacterial activities against XDR-S. Typhi via the agar well diffusion method; 5d has the strongest antibacterial activity with MIC 6.25 (mg/mL). Moreover, in vitro Alkaline Phosphatase inhibitor activity was also determined; 5d is the most potent compound, with an IC50 of 1.469 ± 0.02 µM. Further, in silico studies were performed to find the type of interactions between synthesized compounds and target proteins.
Databáze: Directory of Open Access Journals
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