Evolution of Novel 16-Membered Ketolide Antibiotics:Convergent Synthesis and Biological Evaluation of Tylosin Derivatives
Final Report Abstract
My postdoctoral work in the Myers’ laboratories in the Department of Chemistry and Chemical Biology at Harvard University, Cambridge, MA, USA focussed on the development of novel macrolide antibiotics. This research is highly valuable since the world health system is in demand for new antibiotics in light of the increasing microbial resistance. Within my work, we accomplished the synthesis of twenty complex novel macrolide analogues. Overall, the macrolide-team has synthesized more than 250 new structural analogues. These compounds have been evaluated against a broad panel of pathogens. The examination of the thus obtained MIC data revealed that three new macrolide scaffolds have been identified that show promising activity to overcome microbial resistance against antibiotics.
Publications
- Practical Protocols for the Preparation of Highly Enantioenriched Silyl Ethers of (R)-3-Hydroxypentan-2-one, Building Blocks for the Synthesis of Macrolide Antibiotics. Synlett 2016, 27, 57–60
Ian B. Seiple, Daniel T. Hog, and Andrew G. Myers
(See online at https://doi.org/10.1055/s-0035-1560972) - ‘A Platform for the Discovery of New Macrolide Antibiotics’. Nature volume 533, pages 338–345 (19 May 2016)
Ian B. Seiple, Ziyang Zhang, Pavol Jakubec, Peter M. Wright, Audrey Langlois-Mercier, Daniel T. Hog, Kazuo Yabu, Senkara Allu, Takehiro Fukuzaki, Peter N. Carlsen, Yoshiaki Kitamura, Xiang Zhou, Matthew L. Condakes, Filip T. Szczypiński, William D. Green,
(See online at https://doi.org/10.1038/nature17967)
