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Fragment-based approaches to TB drugs

Published online by Cambridge University Press:  02 November 2016

CHIARA MARCHETTI ,
DANIEL S. H. CHAN ,
ANTHONY G. COYNE  and
CHRIS ABELL
CHIARA MARCHETTI
Affiliation:
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
DANIEL S. H. CHAN
Affiliation:
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
ANTHONY G. COYNE*
Affiliation:
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
CHRIS ABELL*
Affiliation:
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
*
*Corresponding author: Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK. E-mail: [email protected]; [email protected]
*Corresponding author: Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK. E-mail: [email protected]; [email protected]
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Summary

Tuberculosis is an infectious disease associated with significant mortality and morbidity worldwide, particularly in developing countries. The rise of antibiotic resistance in Mycobacterium tuberculosis (Mtb) urgently demands the development of new drug leads to tackle resistant strains. Fragment-based methods have recently emerged at the forefront of pharmaceutical development as a means to generate more effective lead structures, via the identification of fragment molecules that form weak but high quality interactions with the target biomolecule and subsequent fragment optimization. This review highlights a number of novel inhibitors of Mtb targets that have been developed through fragment-based approaches in recent years.

Keywords

tuberculosisfragment-based approachesmedicinal chemistrycytochrome P450pantothenate synthetaseEthRBioA
Type
Special Issue Review
Information
Parasitology , Volume 145 , Special Issue 2: Microbial protein targets: towards understanding and intervention , February 2018 , pp. 184 - 195
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Copyright
Copyright © Cambridge University Press 2016 

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