Tatipaka, Hari Babu; Gillespie, J. Robert; Chatterjee, Arnab K.; Norcross, Neil R.; Hulverson, Matthew A.; Ranade, Ranae M.; Nagendar, Pendem; Creason, Sharon A.; McQueen, Joshua; Duster, Nicole A.; Nagle, Advait; Supek, Frantisek; Molteni, Valentina; Wenzler, Tanja; Brun, Reto; Glynne, Richard; Buckner, Frederick S.; Gelb, Michael H. published the artcile< Substituted 2-Phenylimidazopyridines: A New Class of Drug Leads for Human African Trypanosomiasis>, COA of Formula: C5H6FN3, the main research area is phenylimidazopyridine derivative preparation SAR human trypanosomiasis.
A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of human African trypanosomiasis, led to the identification of substituted 2-(3-aminophenyl)-oxazolopyridines as a starting point for hit-to-lead medicinal chem. A total of 110 analogs were prepared, which led to the identification of I, a substituted 2-(3-aminophenyl)-imidazopyridine. This compound showed antiparasitic activity in vitro with an EC50 of 2 nM and displayed reasonable druglike properties when tested in a number of in vitro assays. I was orally bioavailable and displayed good plasma and brain exposure in mice. I cured mice infected with Trypanosoma brucei when dosed orally down to 2.5 mg/kg. Given its potent antiparasitic properties and its ease of synthesis, I represents a new lead for the development of drugs to treat human African trypanosomiasis.
Journal of Medicinal Chemistry published new progress about Drug bioavailability. 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, COA of Formula: C5H6FN3.