Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, P.R. China.
Chongqing Institute of Green and Intelligent Technology, Chinese Academy of Sciences, Chongqing 400714, China.
Org Lett. 2020 Aug 21;22(16):6632-6636. doi: 10.1021/acs.orglett.0c02403. Epub 2020 Aug 3.
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-ampicillin conjugates, which exhibited more than 500 times improved activity against compared with ampicillin itself. Our studies demonstrate that the vitamin-B uptake pathway could be employed for effective antibiotic delivery and efficacy enhancement.
目前迫切需要发现新的抗生素，并提高现有抗生素对革兰氏阴性菌的疗效。“特洛伊木马”缀合物是一种新颖而有前途的抗生素。在此，我们报告了维生素 B-氨苄青霉素缀合物的设计和合成，与氨苄青霉素本身相比，其对 的活性提高了 500 多倍。我们的研究表明，维生素 B 摄取途径可用于有效递药和增强疗效。
