Anti-malarial activity of N6-modified purine analogues.
Kathleen Too;
Daniel M Brown;
Emily Bongard;
Vanessa Yardley;
Livia Vivas;
David Loakes;
(2007)
Anti-malarial activity of N6-modified purine analogues.
Bioorganic & medicinal chemistry, 15 (16).
pp. 5551-5562.
ISSN 0968-0896
DOI: 10.1016/j.bmc.2007.05.038
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).
| 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 |
| ISI | 248172700020 |