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Molecules 2017, 22(3), 343; doi:10.3390/molecules22030343

Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners

1
Faculty of Chemistry, University of Belgrade, Studentski trg 16, P.O. Box 51, 11158 Belgrade, Serbia
2
Innovation Center of the Faculty of Chemistry, Studentski trg 12-16, 11158 Belgrade, Serbia
3
Institute for Medical Research, University of Belgrade, Dr. Subotića 4, 11129 Belgrade, Serbia
4
Experimental Therapeutics Branch, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 9 January 2017 / Revised: 6 February 2017 / Accepted: 16 February 2017 / Published: 24 February 2017
(This article belongs to the Special Issue Emerging Drug Discovery Approaches against Infectious Diseases)
View Full-Text   |   Download PDF [6848 KB, uploaded 24 February 2017]   |  

Abstract

Malaria is a severe and life-threatening disease caused by Plasmodium parasites that are spread to humans through bites of infected Anopheles mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC50 = 6 nM, and cured 5/5 Plasmodium berghei infected mice when dosed orally at 160 mg/kg/day × 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of <1. This is in sharp contrast to chloroquine, indicating that further development of the series would provide us with more potent antimalarials against CQR strains. View Full-Text
Keywords: antimalarials; thiophene; benzothiophene; aminoquinoline antimalarials; thiophene; benzothiophene; aminoquinoline
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Konstantinović, J.; Videnović, M.; Srbljanović, J.; Djurković-Djaković, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22, 343.

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