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Title: Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials
Authors: Anusha, Sebastian
Sinha, Ameya
Babu Rajeev, C. P.
Chu, Trang T. T.
Mathai, Jessin
Huang, Ximei
Fuchs, Julian E.
Shivananju, NanjundaSwamy
Bender, Andreas
Preiser, Peter Rainer
Rangappa, Kanchugarakoppal S.
Chandramohanadas, Rajesh
Keywords: Drug discovery
Flow cytometry
Plasmodium falciparum
In-vitro screening
Issue Date: 2015
Source: Anusha, S., Sinha, A., Babu Rajeev, C. P., Chu, T. T. T., Mathai, J., Huang, X., et al.. (2015). Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials. Org. Biomol. Chem., 13(43), 10681-10690.
Series/Report no.: Organic & Biomolecular Chemistry
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.
ISSN: 1477-0520
DOI: 10.1039/C5OB01479D
Rights: © 2015 The Royal Society of Chemistry. This is the author created version of a work that has been peer reviewed and accepted for publication by Organic & Biomolecular Chemistry, The Royal Society of Chemistry. It incorporates referee’s comments but changes resulting from the publishing process, such as copyediting, structural formatting, may not be reflected in this document. The published version is available at: [].
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SBS Journal Articles

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