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

doi:10.1002/chem.201701150

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

Biosciences

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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 language	English
Journal	Chemistry: A European Journal
Early online date	4 Apr 2017
DOIs	https://doi.org/10.1002/chem.201701150
Publication status	E-pub ahead of print - 4 Apr 2017

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10.1002/chem.201701150

Dow_et_al_Modular_synthesis_of_diverse_Chemistry_-_A_European_Journal_2017
Checked for eligibility: 10/04/2017. This is the peer reviewed version of the following article:Dow, M., Marchetti, F., Abrahams, K., Vaz, L., Besra, G., Warriner, S. and Nelson, A. (2017), Modular Synthesis of Diverse Natural Product-like Macrocycles: Discovery of Hits with Antimycobacterial Activity. Chem. Eur. J., which has been published in final form at doi:10.1002/chem.201701150. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving.
Accepted author manuscript, 1.52 MBLicence: None: All rights reserved

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

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