Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistan P-falciparum strains. Synthesis and molecular modeling


Gernma, S; Kukreja, G; Campiani, G; Butini, S; Bernetti, M; Joshi, BP; Savini, L; Basifico, N; Taramelli, D; Yardley, V; Bertamino, A; Novellino, E; Persico, M; Catalanotti, B; Fattorusso, C; (2007) Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistan P-falciparum strains. Synthesis and molecular modeling. Bioorganic & medicinal chemistry letters, 17 (13). pp. 3535-3539. ISSN 0960-894X DOI: 10.1016/j.bmcl.2007.04.077

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Abstract

The design, synthesis, and antiplasmodial activity of antimalarial heterodimers based on the 1,4-bis(3-aminopropyl)piperazine linker is reported. In this series key structural elements derived from quinoline antimalarials were coupled to fragments capable of coordinating metal ions. Biological evaluation included determination of activity against chloroquine-sensitive and chloroquine-resistant Plasmodiunifaleiparum strains. Some of the novel compounds presented high activity in vitro against chloroquine-resistant strains, more potent than chloroquine and clotrimazole. Computational studies revealed that the activity is likely due to the ability of the compounds to assume a multisite iron coordinating geometry. (c) 2007 Elsevier Ltd. All rights reserved.

Item Type: Article
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Antimicrobial Resistance Centre (AMR)
Web of Science ID: 247864100002
URI: http://researchonline.lshtm.ac.uk/id/eprint/8435

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