Anti-malarial activity of N6-modified purine analogues

Too, Kathleen, Brown, Daniel M., Bongard, Emily ORCID: https://orcid.org/0000-0001-5957-6280, Yardley, Vanessa, Vivas, Livia and Loakes, David 2007. Anti-malarial activity of N6-modified purine analogues. Bioorganic & Medicinal Chemistry 15 (16) , pp. 5551-5562. 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- (6)-aminoadenosine (2b) and 2-amino-N(6)-amino-N(6)-methyladenosine (4b).

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Medicine
Subjects:	Q Science > QD Chemistry R Medicine > R Medicine (General)
Uncontrolled Keywords:	Purine analogues; Malaria; Tautomerism; Nucleosides; Plasmodium
Publisher:	Elsevier
ISSN:	0968-0896
Last Modified:	25 Oct 2022 08:43
URI:	https://orca.cardiff.ac.uk/id/eprint/54060

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