Synthesis of Vitamin B12-Antibiotic Conjugates with Greatly Improved Activity against Gram-Negative Bacteria
| Autor: | Guoxing Wei, Zhi-Peng Wang, Xumei Wen, Sheng Zhao, Jian Guo, Yun He, Siyu Li |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Gram-negative bacteria
biology 010405 organic chemistry medicine.drug_class Chemistry Organic Chemistry Antibiotics 010402 general chemistry medicine.disease_cause biology.organism_classification 01 natural sciences Biochemistry 0104 chemical sciences Microbiology Ampicillin Antibiotic delivery medicine Vitamin B12 Physical and Theoretical Chemistry Escherichia coli Bacteria medicine.drug Conjugate |
| Zdroj: | Organic Letters. 22:6632-6636 |
| ISSN: | 1523-7052 1523-7060 |
| DOI: | 10.1021/acs.orglett.0c02403 |
| Popis: | There is an urgent need to discover new antibiotics and improve the efficacy of known antibiotics against Gram-negative bacteria. "Trojan horse" conjugates are novel and promising antibiotics. Herein we report the design and synthesis of vitamin-B12-ampicillin conjugates, which exhibited more than 500 times improved activity against Escherichia coli compared with ampicillin itself. Our studies demonstrate that the vitamin-B12 uptake pathway could be employed for effective antibiotic delivery and efficacy enhancement. |
| Databáze: | OpenAIRE |
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