Lin, Cai; Ferreira de Almeida Fiuza, Ludmila; Cardoso Santos, Camila; Ferreira Nunes, Daniela; Cruz Moreira, Otacilio; Bouton, Jakob; Karalic, Izet; Maes, Louis; Caljon, Guy; Hulpia, Fabian; de Nazare C. Soeiro, Maria; Van Calenbergh, Serge published the artcile< 6-Methyl-7-Aryl-7-Deazapurine Nucleosides as Anti-Trypanosoma cruzi Agents: Structure-Activity Relationship and in vivo Efficacy>, Formula: C7H5N3O2, the main research area is purine nucleoside preparation human parasiticide parasitemia prodrug; 7-deazapurine nucleosides; Trypanosoma cruzi; in vivo efficacy; structure-activity relationships.
Chagas disease is a tropical infectious disease resulting in progressive organ-damage and currently lacks efficient treatment and vaccine options. By modifying the pyrimidine part of a previously identified 7-aryl-7-deazapurine nucleoside, we found that substitution of a 6-Me for a 6-amino group allows retaining T. cruzi amastigote growth inhibitory activity but confers improved selectivity towards mammalian cells. The 7-(4-chlorophenyl) analog I, which was stable in microsomes, was evaluated in an acute mouse model. Oral administration of 25 mg/kg b.i.d. suppressed peak parasitemia and protected mice from infection-related mortality, gave similar reductions as the reference drug of blood parasite loads determined by qPCR, but as benznidazole failed to induce sterile cure in the short time period of drug exposure (5 days).
ChemMedChem published new progress about Biological uptake. 101083-92-5 belongs to class indole-building-block, and the molecular formula is C7H5N3O2, Formula: C7H5N3O2.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles