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

Mark Dow, Fransceco Marchetti, Katherine Abrahams, Luis Vaz, Gurdyal Besra, Stuart Warriner

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)
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Abstract

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.

Original languageEnglish
JournalChemistry: A European Journal
Early online date4 Apr 2017
DOIs
Publication statusE-pub ahead of print - 4 Apr 2017

Keywords

  • Journal Article

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