In 2013,Younis, Yassir; Douelle, Frederic; Gonzalez Cabrera, Diego; Le Manach, Claire; Nchinda, Aloysius T.; Paquet, Tanya; Street, Leslie J.; White, Karen L.; Zabiulla, K. Mohammed; Joseph, Jayan T.; Bashyam, Sridevi; Waterson, David; Witty, Michael J.; Wittlin, Sergio; Charman, Susan A.; Chibale, Kelly published 《Structure-Activity-Relationship Studies around the 2 Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity》.Journal of Medicinal Chemistry published the findings.HPLC of Formula: 13534-97-9 The information in the text is summarized as follows:
Replacement of the pyridine core of antimalarial 3,5-diaryl-2-aminopyridines led to the identification of a novel series of pyrazine analogs with potent oral antimalarial activity. However, other changes to the pyridine core and replacement or substitution of the 2-amino group led to loss of antimalarial activity. The 3,5-diaryl-2-aminopyrazine series showed impressive in vitro antiplasmodial activity against the K1 (multidrug resistant) and NF54 (sensitive) strains of Plasmodium falciparum in the nanomolar IC50 range of 6-94 nM while also demonstrating good in vitro metabolic stability in human liver microsomes. In the Plasmodium berghei mouse model, this series generally exhibited good efficacy at low oral doses. One of the frontrunner compounds, (I), displayed potent in vitro antiplasmodial activity with IC50 values of 8.4 and 10 nM against the K1 and NF54 strains, resp. When evaluated in P. berghei-infected mice, compound I was completely curative at an oral dose of 4×10 mg/kg. In the experimental materials used by the author, we found 6-Bromopyridin-3-amine(cas: 13534-97-9HPLC of Formula: 13534-97-9)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.HPLC of Formula: 13534-97-9