دورية أكاديمية
Cholic Acid-Based Antimicrobial Peptide Mimics as Antibacterial Agents
| العنوان: | Cholic Acid-Based Antimicrobial Peptide Mimics as Antibacterial Agents |
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| المؤلفون: | Jie Wu, Tsz Tin Yu, Rajesh Kuppusamy, Md. Musfizur Hassan, Amani Alghalayini, Charles G. Cranfield, Mark D. P. Willcox, David StC. Black, Naresh Kumar |
| المصدر: | International Journal of Molecular Sciences, Vol 23, Iss 9, p 4623 (2022) |
| بيانات النشر: | MDPI AG, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Biology (General) LCC:Chemistry |
| مصطلحات موضوعية: | cholic acid, antimicrobial peptide, peptidomimetics, antibacterial, membrane disruption, Biology (General), QH301-705.5, Chemistry, QD1-999 |
| الوصف: | There is a significant and urgent need for the development of novel antibacterial agents to tackle the increasing incidence of antibiotic resistance. Cholic acid-based small molecular antimicrobial peptide mimics are reported as potential new leads to treat bacterial infection. Here, we describe the design, synthesis and biological evaluation of cholic acid-based small molecular antimicrobial peptide mimics. The synthesis of cholic acid analogues involves the attachment of a hydrophobic moiety at the carboxyl terminal of the cholic acid scaffold, followed by the installation of one to three amino acid residues on the hydroxyl groups present on the cholic acid scaffold. Structure–activity relationship studies suggest that the tryptophan moiety is important for high antibacterial activity. Moreover, a minimum of +2 charge is also important for antimicrobial activity. In particular, analogues containing lysine-like residues showed the highest antibacterial potency against Gram-positive S. aureus. All di-substituted analogues possess high antimicrobial activity against both Gram-positive S. aureus as well as Gram-negative E. coli and P. aeruginosa. Analogues 17c and 17d with a combination of these features were found to be the most potent in this study. These compounds were able to depolarise the bacterial membrane, suggesting that they are potential antimicrobial pore forming agents. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1422-0067 1661-6596 |
| Relation: | https://www.mdpi.com/1422-0067/23/9/4623; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067 |
| DOI: | 10.3390/ijms23094623 |
| URL الوصول: | https://doaj.org/article/bc736b1d103244eb8d6b22793d0352fe |
| رقم الأكسشن: | edsdoj.bc736b1d103244eb8d6b22793d0352fe |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14220067 16616596 |
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| DOI: | 10.3390/ijms23094623 |