1314882-73-9Relevant articles and documents
Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines
González Cabrera, Diego,Douelle, Frederic,Younis, Yassir,Feng, Tzu-Shean,Le Manach, Claire,Nchinda, Aloysius T.,Street, Leslie J.,Scheurer, Christian,Kamber, Jolanda,White, Karen L.,Montagnat, Oliver D.,Ryan, Eileen,Katneni, Kasiram,Zabiulla, K. Mohammed,Joseph, Jayan T.,Bashyam, Sridevi,Waterson, David,Witty, Michael J.,Charman, Susan A.,Wittlin, Sergio,Chibale, Kelly
, p. 11022 - 11030 (2012)
In an effort to address potential cardiotoxicity liabilities identified with earlier frontrunner compounds, a number of new 3,5-diaryl-2-aminopyridine derivatives were synthesized. Several compounds exhibited potent antiplasmodial activity against both the multidrug resistant (K1) and sensitive (NF54) strains in the low nanomolar range. Some compounds displayed a significant reduction in potency in the hERG channel inhibition assay compared to previously reported frontrunner analogues. Several of these new analogues demonstrated promising in vivo efficacy in the Plasmodium berghei mouse model and will be further evaluated as potential clinical candidates. The SAR for in vitro antiplasmodial and hERG activity was delineated.
NEW ANTI-MALARIAL AGENTS
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Page/Page column 46, (2011/08/04)
The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharm
