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

Anusha, S. and Sinha, A. and Rajeev, C. P. B. and Chu, T. T. T. and Mathai, J. and Ximei, H. and Fuchs, J. E. and Shivananju, N. S. and Bender, A. and Preiser, P. R. and Rangappa, K. S. and Basappa and Chandramohanadas, R. (2015) Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials. ORGANIC & BIOMOLECULAR CHEMISTRY, 13 (43). pp. 10681-10690. ISSN 1477-0539

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Official URL: https://doi.org/10.1039/c5ob01479d

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-myristoyl-transferase 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.

Item Type: Article
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Shrirekha N
Date Deposited: 18 Jun 2019 05:06
Last Modified: 18 Jun 2019 05:06
URI: http://eprints.uni-mysore.ac.in/id/eprint/3244

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