Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivo antimalarial activities
Francesc Marti;
James Chadwick;
Richard K Amewu;
Hollie Burrell-Saward;
Abhishek Srivastava;
Stephen A Ward;
Raman Sharma;
Neil Berry;
Paul M O'Neill;
(2011)
Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivo antimalarial activities.
MedChemComm, 2 (7).
p. 661.
ISSN 2040-2503
DOI: 10.1039/c1md00102g
A series of polar dispiro-1,2,4,5-tetraoxanes have been designed and synthesized by parallel synthesis. From this series, endoperoxides with activity as low as 0.2 nM have been obtained and representatives of this group have excellent oral activities in the P. berghei ANKA mouse model of malaria. © 2011 The Royal Society of Chemistry.
| Item Type | Article |
|---|---|
| Keywords | drug-development candidate, crystal-structure, dispiro-1, 2, 4, 5-tetraoxanes, artemisinin, peroxides, spiro-1, 2, 4, 5-tetraoxacycloalkanes, 1, 2, 4, 5-tetraoxane, identification, mechanism, malaria |
| ISI | 293316800016 |