Benzothiophene Carboxamide Derivatives as Novel Antimalarials

Banerjee, Tanushree and Kapoor, Neha and Surolia, Namita and Surolia, Avadhesha (2011) Benzothiophene Carboxamide Derivatives as Novel Antimalarials. In: IUBMB Life, 63 (12). pp. 1111-1115.

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Abstract

Bromo-benzothiophene carboxamide derivatives have been shown in the preceding article to inhibit Plasmodium falciparum Enoyl-ACP reductase. Here, we report bromo-benzothiophene carboxamide derivatives as potent inhibitors of Plasmodium asexual blood-stages in vitro as well as in vivo in the mouse model. These compounds specifically impair the development of metabolically active trophozoite stage of intraerythrocytic cycle and the intravenous administration of 3-bromo-N-(4-fluorobenzyl)-benzo[b]thiophene-2-carboxamide (compound 6) enhances the longevity of P. berghei infected mice by 2 weeks compared to disease control animals thereby preventing the onset of ataxia and convulsions in treated mice. These compounds thus hold promise for the development of potent antimalarials.(C) 2011 IUBMB IUBMB Life, 63(12): 1111-1115, 2011

Item Type:	Journal Article
Publication:	IUBMB Life
Publisher:	John Wiley and Sons
Additional Information:	Copyright of this article belongs to John Wiley and Sons.
Keywords:	benzothiophene;benzothiophene carboxamide;antimalarials; Plasmodium
Department/Centre:	Division of Biological Sciences > Molecular Biophysics Unit
Date Deposited:	10 Jan 2012 12:28
Last Modified:	10 Jan 2012 12:28
URI:	http://eprints.iisc.ac.in/id/eprint/43110

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