1309358-75-5Relevant 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.
AMINO ARYL ACETAMIDES AND THEIR USE IN THE TREATMENT OF MALARIA
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Page/Page column 40, (2011/06/19)
Amino phenyl acetamide compounds of Formula (I):and pharmaceutically acceptable salts thereof: wherein R1, R2, R3 and Ra are as defined in the description, use of such compounds in the chemotherapy of certain parasitic protozoal infections such as malaria, pharmaceutical compositions including such compounds and processes for the preparation of such compounds, are provided.
