Anti-malarial activity of N-6-modified purine analogues


Too, K; Brown, DM; Bongard, E; Yardley, V; Vivas, L; Loakes, D; (2007) Anti-malarial activity of N-6-modified purine analogues. Bioorganic & medicinal chemistry, 15 (16). pp. 5551-5562. ISSN 0968-0896 DOI: https://doi.org/10.1016/j.bmc.2007.05.038

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Abstract

Plasmodium falciparum causes one of the deadliest forms of malaria and resistance to the currently available drugs makes it imperative to develop new, safe and potent drugs. Parasites such as P. falciparum are unable to synthesise purines de novo and to this end often have multiple purine uptake and salvage systems. With this in mind, we have designed and synthesised libraries of purine analogues as potential anti-malarial agents. Herein, we report three compounds with promising activity against the highly chloroquine-resistant VS1 P. falciparum namely: N-6-hydroxyadenine (1c), 2-amino-N-6-aminoadenosine (2b) and 2-amino-N-6-amino-N-6-methyladenosine (4b). (c) 2007 Elsevier Ltd. All rights reserved.

Item Type: Article
Keywords: Animals, Antimalarials, chemical synthesis, chemistry, toxicity, Male, Mice, Molecular Structure, Plasmodium falciparum, drug effects, Purines, chemical synthesis, chemistry, toxicity, Structure-Activity Relationship
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Malaria Centre
PubMed ID: 17548196
Web of Science ID: 248172700020
URI: http://researchonline.lshtm.ac.uk/id/eprint/8433

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