53215-12-6Relevant articles and documents
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi
Santos, Camila C.,Lionel, Jéssica R.,Peres, Raiza B.,Batista, Marcos M.,Da Silva, Patrícia B.,De Oliveira, Gabriel M.,Da Silva, Cristiane F.,Batista, Denise G. J.,Souza, Sandra Maria O.,Andrade, Carolina H.,Neves, Bruno J.,Braga, Rodolpho C.,Patrick, Donald A.,Bakunova, Svetlana M.,Tidwell, Richard R.,Soeiro, Maria de Nazaré C.
supporting information, (2018/02/06)
Five bis-arylimidamides were assayed as anti-Trypanosoma cruzi agents by in vitro, in silico, and in vivo approaches. None were considered to be pan-assay interference compounds. They had a favorable pharmacokinetic landscape and were active against trypomastigotes and intracellular forms, and in combination with benznidazole, they gave no interaction. The most selective agent (28SMB032) tested in vivo led to a 40% reduction in parasitemia (0.1 mg/kg of body weight/5 days intraperitoneally) but without mortality protection. In silico target fishing suggested DNA as the main target, but ultrastructural data did not match.
A convenient preparation of 3,5-diarylisoxazoles
Wei,Fang,Hu,Hu
, p. 1205 - 1206 (2007/10/02)
3,5-Diarylisoxazoles 2a-i were prepared in moderate to high yields 51-94%) by oxidation of chalcone oximes with a new metal complex oxidant, tetrakis(pyridine)cobalt(II) dichromate (TPCD).
