3 years ago

Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity

Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity
Luis Vaz, Francesco Marchetti, Katherine A. Abrahams, Adam Nelson, Stuart Warriner, Mark Dow, Gurdyal S. Besra
A modular synthetic approach was developed in which variation of the triplets of building blocks used enabled systematic variation of the macrocyclic scaffolds prepared. The approach was demonstrated in the synthesis of 17 diverse natural product-like macrocyclic scaffolds of varied (12–20-membered) ring size. The biological relevance of the chemical space explored was demonstrated through the discovery of a series of macrocycles with significant antimycobacterial activity. A modular approach enabled the synthesis of 17 diverse natural product-like macrocyclic scaffolds, and the discovery of a distinctive macrocycles with antimycobacterial activity.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201701150

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