title: Anti-malarial activity of N6-modified purine analogues.
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).
authors.affiliation: Medical Research Council, Laboratory of Molecular Biology, Hills Road, Cambridge CB2 2QH, UK.
authors.forename: Kathleen
authors.initials: K
authors.lastname: Too
authors.forename: Daniel M
authors.initials: DM
authors.lastname: Brown
authors.forename: Emily
authors.initials: E
authors.lastname: Bongard
authors.forename: Vanessa
authors.initials: V
authors.lastname: Yardley
authors.forename: Livia
authors.initials: L
authors.lastname: Vivas
authors.forename: David
authors.initials: D
authors.lastname: Loakes
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011687:Purines; C030985:purine