Improving Nature’s antibiotics through (semi)synthesis
Prof.
dr.
Nathaniel
I.
Martin
Biological
Chemistry
Group
Institute
of
Biology
Leiden,
Leiden University
Leiden,
The
Netherlands
Wednesday,
May
24,
2023
2:30
p.m.
In-person: C2- 361 (Reading Room)
Abstract: The development of next-generation antibiotics with enhanced activity, reduced toxicity, and the capacity to overcome resistance is a growing challenge for the medical community. To address this challenge, the Martin group has recently applied chemistry-based strategies to enhance the properties of the naturally occurring antibiotics vancomycin and bacitracin. Using both semi-synthesis and total synthesis approaches, novel analogues of vancomycin and bacitracin were prepared and found to exhibit potent activity against a range of Gram-positive pathogens. The ability of these new analogues to inhibit bacterial cell wall synthesis was also confirmed using a variety of biochemical assays. Notably, these new analogues are significantly more active than vancomycin and bacitracin and are also highly effective in vivo. Also of note is the ability of these next-generation antibiotics to overcome many clinically relevant resistance mechanisms.