849900-16-9Relevant academic research and scientific papers
Cyclopropyl carboxamides: A new oral antimalarial series derived from the Tres Cantos Anti-Malarial Set (TCAMS)
Rueda, Lourdes,Castellote, Isabel,Castro-Pichel, Julia,Chaparro, Maria J.,De La Rosa, Juan Carlos,Garcia-Perez, Adolfo,Gordo, Mariola,Jimenez-Diaz, Maria Belen,Kessler, Albane,MacDonald, Simon J.F.,Martinez, Maria Santos,Sanz, Laura M.,Gamo, Francisco Javier,Fernandez, Esther
supporting information; experimental part, p. 840 - 844 (2012/01/05)
Rapid triaging of three series of related hits selected from the Tres Cantos Anti-Malarial Set (TCAMS) are described. A triazolopyrimidine series was deprioritized due to delayed inhibition of parasite growth. A lactic acid series has derivatives with IC50 50 = 3 nM) and has an oral bioavailability of 55% in CD-1 mice and an ED90 of 20 mg/kg after oral dosing in a nonmyelo-depleted P. falciparum murine model.
