Professor Yun He's team makes important progress in improving activity against Gram-negative bacteria

Antibiotics are rapidly losing their antimicrobial efficacy due to their overuse and misuse worldwide, hence the situation is particularly critical for Gram-negative bacteria and to meet this challenge. To address this challenge, “Trojan horse” couples have emerged as a promising new antibiotic. In a review of the literature, Professor Yun He and Jian Guo found that vitamin B₁₂ is an essential nutrient for mammalian and many bacterial cells, most bacteria require vitamin B₁₂ to grow, and most of them must extract vitamin B₁₂ from their host or environment via active transport. The design and synthesis of a vitamin B₁₂-aminobenzyl penicillin conjugate was carried out by Yun He's group to address these challenges, and the conjugate was more than 500-fold more active against E. coli compared to benzylpenicillin itself. It was also demonstrated that the vitamin B₁₂ uptake pathway could effectively enhance antibiotic delivery and efficacy.

Links to the paper: https://pubs.acs.org/doi/abs/10.1021/acs.orglett.0c02403

DOI: 10.1021/acs.orglett.0c02403