Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/54466
Title: Antiplasmodial, beta-haematin inhibition, antitrypanosomal and cytotoxic activity in vitro of novel 4-aminoquinoline 2-imidazolines
Authors: Musonda, Chitalu C.
Yardley, Vanessa
Souza, Renata Celi Carvalho de
Ncokazi, Kanyile
Egan, Timothy J.
Chibale, Kelly
Affilliation: Department of Chemistry. University of Cape Town. Rondebosch,South Africa.
Department of Infectious & Tropical Diseases. London School of Hygieneand Tropical Medicine. London, WC, UK
Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brazil
Department of Chemistry. University of Cape Town. Rondebosch,South Africa.
Department of Chemistry. University of Cape Town. Rondebosch,South Africa.
Department of Chemistry. University of Cape Town. Rondebosch,South Africa/Institute of Infectious Disease and Molecular Medicine, University of CapeTown Medical School. Observatory, South Africa
Abstract: A novel series of 4-aminoquinoline-containing 2-imidazolines were synthesized via a one-pot 3-component condensation reaction of amine, aldehyde and isocyanoacetate. The products were obtained in high yield as well as purity and were evaluated directly against two strains of Plasmodium falciparum and Trypanosoma brucei. Compound 21 was the most active across all parasites with ED50 = 3.3 nM against a chloroquine (CQ)-sensitive 3D7 strain, ED50 = 33 nM against a CQ-resistant K1 strain and ED50 = 70 nM against T. brucei. Several compounds were able to inhibit formation of beta-haematin in vitro, suggesting haemozoin formation in the malaria parasite as a possible target. On the other hand, evaluation against a human KB cell line revealed that the compounds were generally non-cytotoxic to the host cells
Issue Date: 2008
Publisher: Royal Society of Chemistry
Citation: MUSONDA, Chitalu C et al. Antiplasmodial, beta-haematin inhibition, antitrypanosomal and cytotoxic activity in vitro of novel 4-aminoquinoline 2-imidazolines. Org Biomol Chem.,v. 6, n. 23, p. 4446-4451, 2008. doi: 10.1039/b813007h.
DOI: 10.1039/b813007h
ISSN: 1477-0520
Copyright: restricted access
Appears in Collections:MG - IRR - Artigos de Periódicos
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