74188-45-7Relevant articles and documents
Antimalarial activities of new guanidylimidazole and guanidylimidazoline derivatives
Zhang, Liang,Sathunuru, Ramadas,Caridha, Diana,Pybus, Brandon,O'Neil, Michael T.,Kozar, Michael P.,Lin, Ai J.
, p. 6634 - 6646 (2011)
A series of new guanidylimidazole derivatives was prepared and evaluated in mice and Rhesus monkeys infected with malarial sporozoites. The majority of the new compounds showed poor metabolic stability and weak in vitro activities in three clones of Plasm
Synthesis and antimalarial activity of 2-guanidino-4-oxoimidazoline derivatives
Liu, Xianjun,Wang, Xihong,Li, Qigui,Kozar, Michael P.,Melendez, Victor,O Neil, Michael T.,Lin, Ai J.
experimental part, p. 4523 - 4535 (2011/09/15)
A series of 2-guanidino-4-oxoimidazoline (deoxo-IZ) derivatives was prepared and showed potent antimalarial activities in rodent and Rhesus models. Compound 8e, the most potent analogues of this series, is the first non-8-aminoqinoline antimalarial that demonstrated radical curative activity in non-human primate by oral route and showed causal prophylactic activity comparable to that of the commonly used clinical drugs in Rhesus monkeys infected with sporozoites of Plasmodium cynomolgi. The metabolic stability and metabolites profile indicated that the new deoxo-IZ derivatives (8) may act as prodrugs of the corresponding IZ (1 and 2) derivatives.
