Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/81894
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dc.contributor.authorAnusha, Sebastianen
dc.contributor.authorSinha, Ameyaen
dc.contributor.authorBabu Rajeev, C. P.en
dc.contributor.authorChu, Trang T. T.en
dc.contributor.authorMathai, Jessinen
dc.contributor.authorHuang, Ximeien
dc.contributor.authorFuchs, Julian E.en
dc.contributor.authorShivananju, NanjundaSwamyen
dc.contributor.authorBender, Andreasen
dc.contributor.authorPreiser, Peter Raineren
dc.contributor.authorRangappa, Kanchugarakoppal S.en
dc.contributor.authorBasappaen
dc.contributor.authorChandramohanadas, Rajeshen
dc.date.accessioned2016-01-21T04:22:12Zen
dc.date.accessioned2019-12-06T14:42:32Z-
dc.date.available2016-01-21T04:22:12Zen
dc.date.available2019-12-06T14:42:32Z-
dc.date.issued2015en
dc.identifier.citationAnusha, 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.en
dc.identifier.issn1477-0520en
dc.identifier.urihttps://hdl.handle.net/10356/81894-
dc.description.abstractMalaria 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.en
dc.description.sponsorshipNRF (Natl Research Foundation, S’pore)en
dc.description.sponsorshipMOE (Min. of Education, S’pore)en
dc.format.extent23 p.en
dc.language.isoenen
dc.relation.ispartofseriesOrganic & Biomolecular Chemistryen
dc.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].en
dc.subjectDrug discoveryen
dc.subjectGiemsa-stainingen
dc.subjectMicroscopyen
dc.subjectFlow cytometryen
dc.subjectAnti-malarialsen
dc.subjectPlasmodium falciparumen
dc.subjectIn-vitro screeningen
dc.titleSynthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarialsen
dc.typeJournal Articleen
dc.contributor.schoolSchool of Biological Sciencesen
dc.identifier.doi10.1039/C5OB01479Den
dc.description.versionAccepted versionen
item.grantfulltextopen-
item.fulltextWith Fulltext-
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