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Org Biomol Chem. 2015 Nov 21;13(43):10681-90. doi: 10.1039/c5ob01479d.

Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials.

Author information

1
Laboratory of Chemical Biology, Department of Chemistry, Bangalore University, Bangalore, India. salundibasappa@gmail.com.
2
Pillar of Engineering Product Development, Singapore University of Technology & Design, Singapore. rajesh@sutd.edu.sg.
3
Gulf Medical University, Ajman, United Arab Emirates.
4
School of Biological Sciences, Nanyang Technological University, Singapore.
5
Centre for Molecular Science Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, UK and Institute of General, Inorganic and Theoretical Chemistry, University of Innsbruck, Innrain 82, 6020 Innsbruck, Austria.
6
Department of Studies in Chemistry, University of Mysore, Mysore, India.
7
Centre for Molecular Science Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, UK.

Abstract

Malaria parasites are currently gaining drug-resistance rapidly, across countries and continents. Hence, the discovery and development of novel chemical scaffolds, with superior antimalarial activity remain an important priority, for the developing world. Our report describes the development, characterization and evaluation of novel bepotastine-based sulphonamide antimalarials inhibiting asexual stage development of Plasmodium falciparum parasites in vitro. The screening results showed potent inhibitory activity of a number of novel sulphonamides against P. falciparum at low micromolar concentrations, in particular in late-stage parasite development. Based on computational studies we hypothesize N-myristoyltransferase as the target of the compounds developed here. Our results demonstrate the value of novel bepotastine-based sulphonamide compounds for targeting the asexual developmental stages of P. falciparum.

PMID:
26347024
DOI:
10.1039/c5ob01479d
[Indexed for MEDLINE]

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