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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: N6-hydroxyadenine (1c), 2-amino-N6-aminoadenosine (2b) and 2-amino-N6-amino-N6-methyladenosine (4b). © 2007 Elsevier Ltd. All rights reserved.

Original publication

DOI

10.1016/j.bmc.2007.05.038

Type

Journal article

Journal

Bioorganic and Medicinal Chemistry

Publication Date

15/08/2007

Volume

15

Pages

5551 - 5562