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Synthesis of Vitamin B-12-Antibiotic Conjugates with Greatly Improved Activity against Gram-Negative Bacteria
Zhao, Sheng1; Wang, Zhi-Peng2; Wen, Xumei1; Li, Siyu1; Wei, Guoxing1; Guo, Jian1; He, Yun1
2020-08-21
摘要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-B-12-ampicillin conjugates, which exhibited more than 500 times improved activity against Escherichia coli compared with ampicillin itself. Our studies demonstrate that the vitamin-B-12 uptake pathway could be employed for effective antibiotic delivery and efficacy enhancement.
DOI10.1021/acs.orglett.0c02403
发表期刊ORGANIC LETTERS
ISSN1523-7060
卷号22期号:16页码:6632-6636
通讯作者Guo, Jian(jian.guo@cqu.edu.cn) ; He, Yun(yun.he@cqu.edu.cn)
收录类别SCI
WOS记录号WOS:000563755700080
语种英语