Open Access
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
Abdul Hannan Khan
1
,
Muhammad Bilal
1
,
Abid Mahmood
2
,
Nasir Rasool
1
,
Muhammad Usman Qamar
3
,
Muhammad Imran
4
,
Sebastian Ionut Toma
5
,
Oana Andreescu
5
Publication type: Journal Article
Publication date: 2024-09-20
PubMed ID:
39338403
Abstract
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.
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Total citations:
4
Citations from 2024:
4
(100%)
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Khan A. H. et al. 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 // Pharmaceuticals. 2024. Vol. 17. No. 9. p. 1241.
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Khan A. H., Bilal M., Mahmood A., Rasool N., Qamar M. U., Imran M., Toma S. I., Andreescu O. 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 // Pharmaceuticals. 2024. Vol. 17. No. 9. p. 1241.
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RIS
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TY - JOUR
DO - 10.3390/ph17091241
UR - https://www.mdpi.com/1424-8247/17/9/1241
TI - 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
T2 - Pharmaceuticals
AU - Khan, Abdul Hannan
AU - Bilal, Muhammad
AU - Mahmood, Abid
AU - Rasool, Nasir
AU - Qamar, Muhammad Usman
AU - Imran, Muhammad
AU - Toma, Sebastian Ionut
AU - Andreescu, Oana
PY - 2024
DA - 2024/09/20
PB - MDPI
SP - 1241
IS - 9
VL - 17
PMID - 39338403
SN - 1424-8247
ER -
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BibTex (up to 50 authors)
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@article{2024_Khan,
author = {Abdul Hannan Khan and Muhammad Bilal and Abid Mahmood and Nasir Rasool and Muhammad Usman Qamar and Muhammad Imran and Sebastian Ionut Toma and Oana Andreescu},
title = {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},
journal = {Pharmaceuticals},
year = {2024},
volume = {17},
publisher = {MDPI},
month = {sep},
url = {https://www.mdpi.com/1424-8247/17/9/1241},
number = {9},
pages = {1241},
doi = {10.3390/ph17091241}
}
Cite this
MLA
Copy
Khan, Abdul Hannan, et al. “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.” Pharmaceuticals, vol. 17, no. 9, Sep. 2024, p. 1241. https://www.mdpi.com/1424-8247/17/9/1241.