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|Title:||Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials||Authors:||Anusha, Sebastian
Babu Rajeev, C. P.
Chu, Trang T. T.
Fuchs, Julian E.
Preiser, Peter Rainer
Rangappa, Kanchugarakoppal S.
|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.||URI:||https://hdl.handle.net/10356/81894
|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: [http://dx.doi.org/10.1039/C5OB01479D].||Fulltext Permission:||open||Fulltext Availability:||With Fulltext|
|Appears in Collections:||SBS Journal Articles|
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