Background: To highlight the magnitude of the important challenge now facing scientists, drug resistance needs exploration of novel antimicrobial agents. The identification of new and vital target in bacteria and then designing their inhibitors can be explored. Thus, targeting SecA, a central component of the bacterial general secretion system, is a promising strategy for the development of novel antimicrobials. Objective: To evaluate new compounds as SecA inhibitors synthesized by structural modification of bistriazole SCA-21. Method: A new compounds were synthesized and evaluated for antibacterial activity against Escherichia coli NR698 (E. coli a leaky mutant), Staphylococcus aureus (S. aureus) and Bacillus anthracis (B. anthracis). Results: Some novel triazole-pyrimidine derivatives by structural modification of known SecA inhibitor SCA 21 were synthesized and their structures were confirmed by 1H NMR, 13C NMR and Mass spectral analysis. The synthesized compound showed antimicrobial activity against E. coli NR698 (a leaky mutant), S. aureus and B. anthracis Sterne. Conclusion: Five novel triazole-pyrimidine derivatives were designed, synthesized and evaluated as SecA inhibitors. At the end of this study, compound SCA 259 with azide pentyl group was found as the most potent inhibitor. It expressed better inhibitory activity against SecA ATPase than else known inhibitor SCA 21.
| Published in | Advances in Biochemistry (Volume 9, Issue 4) |
| DOI | 10.11648/j.ab.20210904.12 |
| Page(s) | 98-105 |
| Creative Commons |
This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited. |
| Copyright |
Copyright © The Author(s), 2021. Published by Science Publishing Group |
Triazole-Pyrimidine, SecA Inhibitor, Small Molecule, Antimicrobial, Target, Drug-resistant
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APA Style
Fanté Bamba, Camara Tchambaga Etienne, Coulibali Sioménan, Akpa Sagne Jacques, Coulibaly Souleymane, et al. (2021). Design, Synthesis and Antibacterial Activities of Triazole-Pyrimidine Derivatives as SecA Inhibitors. Advances in Biochemistry, 9(4), 98-105. https://doi.org/10.11648/j.ab.20210904.12
ACS Style
Fanté Bamba; Camara Tchambaga Etienne; Coulibali Sioménan; Akpa Sagne Jacques; Coulibaly Souleymane, et al. Design, Synthesis and Antibacterial Activities of Triazole-Pyrimidine Derivatives as SecA Inhibitors. Adv. Biochem. 2021, 9(4), 98-105. doi: 10.11648/j.ab.20210904.12
AMA Style
Fanté Bamba, Camara Tchambaga Etienne, Coulibali Sioménan, Akpa Sagne Jacques, Coulibaly Souleymane, et al. Design, Synthesis and Antibacterial Activities of Triazole-Pyrimidine Derivatives as SecA Inhibitors. Adv Biochem. 2021;9(4):98-105. doi: 10.11648/j.ab.20210904.12
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Download@article{10.11648/j.ab.20210904.12,
author = {Fanté Bamba and Camara Tchambaga Etienne and Coulibali Sioménan and Akpa Sagne Jacques and Coulibaly Souleymane and Adjou Ané},
title = {Design, Synthesis and Antibacterial Activities of Triazole-Pyrimidine Derivatives as SecA Inhibitors},
journal = {Advances in Biochemistry},
volume = {9},
number = {4},
pages = {98-105},
doi = {10.11648/j.ab.20210904.12},
url = {https://doi.org/10.11648/j.ab.20210904.12},
eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.ab.20210904.12},
abstract = {Background: To highlight the magnitude of the important challenge now facing scientists, drug resistance needs exploration of novel antimicrobial agents. The identification of new and vital target in bacteria and then designing their inhibitors can be explored. Thus, targeting SecA, a central component of the bacterial general secretion system, is a promising strategy for the development of novel antimicrobials. Objective: To evaluate new compounds as SecA inhibitors synthesized by structural modification of bistriazole SCA-21. Method: A new compounds were synthesized and evaluated for antibacterial activity against Escherichia coli NR698 (E. coli a leaky mutant), Staphylococcus aureus (S. aureus) and Bacillus anthracis (B. anthracis). Results: Some novel triazole-pyrimidine derivatives by structural modification of known SecA inhibitor SCA 21 were synthesized and their structures were confirmed by 1H NMR, 13C NMR and Mass spectral analysis. The synthesized compound showed antimicrobial activity against E. coli NR698 (a leaky mutant), S. aureus and B. anthracis Sterne. Conclusion: Five novel triazole-pyrimidine derivatives were designed, synthesized and evaluated as SecA inhibitors. At the end of this study, compound SCA 259 with azide pentyl group was found as the most potent inhibitor. It expressed better inhibitory activity against SecA ATPase than else known inhibitor SCA 21.},
year = {2021}
}
TY - JOUR T1 - Design, Synthesis and Antibacterial Activities of Triazole-Pyrimidine Derivatives as SecA Inhibitors AU - Fanté Bamba AU - Camara Tchambaga Etienne AU - Coulibali Sioménan AU - Akpa Sagne Jacques AU - Coulibaly Souleymane AU - Adjou Ané Y1 - 2021/11/23 PY - 2021 N1 - https://doi.org/10.11648/j.ab.20210904.12 DO - 10.11648/j.ab.20210904.12 T2 - Advances in Biochemistry JF - Advances in Biochemistry JO - Advances in Biochemistry SP - 98 EP - 105 PB - Science Publishing Group SN - 2329-0862 UR - https://doi.org/10.11648/j.ab.20210904.12 AB - Background: To highlight the magnitude of the important challenge now facing scientists, drug resistance needs exploration of novel antimicrobial agents. The identification of new and vital target in bacteria and then designing their inhibitors can be explored. Thus, targeting SecA, a central component of the bacterial general secretion system, is a promising strategy for the development of novel antimicrobials. Objective: To evaluate new compounds as SecA inhibitors synthesized by structural modification of bistriazole SCA-21. Method: A new compounds were synthesized and evaluated for antibacterial activity against Escherichia coli NR698 (E. coli a leaky mutant), Staphylococcus aureus (S. aureus) and Bacillus anthracis (B. anthracis). Results: Some novel triazole-pyrimidine derivatives by structural modification of known SecA inhibitor SCA 21 were synthesized and their structures were confirmed by 1H NMR, 13C NMR and Mass spectral analysis. The synthesized compound showed antimicrobial activity against E. coli NR698 (a leaky mutant), S. aureus and B. anthracis Sterne. Conclusion: Five novel triazole-pyrimidine derivatives were designed, synthesized and evaluated as SecA inhibitors. At the end of this study, compound SCA 259 with azide pentyl group was found as the most potent inhibitor. It expressed better inhibitory activity against SecA ATPase than else known inhibitor SCA 21. VL - 9 IS - 4 ER -
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