N-methyl Benzimidazole Tethered Cholic Acid Amphiphiles Can Eradicate S. aureus-Mediated Biofilms and Wound Infections
Abstract
:1. Introduction
2. Results and Discussion
2.1. Design and Synthesis of CA-Benzimidazole Amphiphiles
2.2. Antibacterial Activities of CA-Benzimidazole Amphiphiles
2.3. CABI-6 Amphiphile Is Bactericidal
2.4. CABI-6 Amphiphile Can Disrupt the Bacterial Membranes
2.5. CABI-6 Can Eradicate the Preformed S. aureus Biofilms
2.6. CABI-6 can Mitigate the S. aureus-Mediated Murine Wound Infection
3. Experimental Section
3.1. Materials
3.2. Synthesis of Cholic Acid Esters (10a–10h)
3.3. Synthesis of Chloroacetylated Cholic Acid Esters (11a–11h)
3.4. Synthesis of CABI Amphiphiles
3.5. Material and Methods
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Minimum Inhibitory Concentration (MIC99) (μg/mL) | ||||||||
---|---|---|---|---|---|---|---|---|
Gram-Positive Strains | Gram-Negative Strains | |||||||
S. aureus | S. pneumoniae | B. subtilis | S. oralis | E. Coli | P. aeruginosa | K. pneumoniae | S. typhimurium | |
CABI-1 | >128 | >128 | >128 | 8 | >128 | >128 | >128 | >128 |
CABI-2 | 128 | 128 | 128 | 4 | >128 | >128 | >128 | >128 |
CABI-3 | 128 | 128 | 128 | 4 | >128 | 128 | >128 | >128 |
CABI-4 | 32 | 32 | 64 | 2 | >128 | 64 | >128 | >128 |
CABI-5 | 32 | 32 | 128 | 2 | >128 | 32 | >128 | >128 |
CABI-6 | 16 | 32 | 128 | 2 | >128 | 32 | >128 | >128 |
CABI-7 | 16 | 32 | 64 | 2 | >128 | 16 | >128 | 128 |
CABI-8 | 32 | 32 | 32 | 2 | >128 | 32 | >128 | >128 |
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Kakkar, H.; Chaudhary, N.; Mehta, D.; Saini, V.; Maheshwari, S.; Singh, J.; Walia, P.; Bajaj, A. N-methyl Benzimidazole Tethered Cholic Acid Amphiphiles Can Eradicate S. aureus-Mediated Biofilms and Wound Infections. Molecules 2022, 27, 3501. https://doi.org/10.3390/molecules27113501
Kakkar H, Chaudhary N, Mehta D, Saini V, Maheshwari S, Singh J, Walia P, Bajaj A. N-methyl Benzimidazole Tethered Cholic Acid Amphiphiles Can Eradicate S. aureus-Mediated Biofilms and Wound Infections. Molecules. 2022; 27(11):3501. https://doi.org/10.3390/molecules27113501
Chicago/Turabian StyleKakkar, Himanshu, Nalini Chaudhary, Devashish Mehta, Varsha Saini, Shallu Maheshwari, Jitender Singh, Preeti Walia, and Avinash Bajaj. 2022. "N-methyl Benzimidazole Tethered Cholic Acid Amphiphiles Can Eradicate S. aureus-Mediated Biofilms and Wound Infections" Molecules 27, no. 11: 3501. https://doi.org/10.3390/molecules27113501