Ontology highlight
ABSTRACT:
SUBMITTER: Comer E
PROVIDER: S-EPMC4207553 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20141013 20
Here, we describe medicinal chemistry that was accelerated by a diversity-oriented synthesis (DOS) pathway, and in vivo studies of our previously reported macrocyclic antimalarial agent that derived from the synthetic pathway. Structure-activity relationships that focused on both appendage and skeletal features yielded a nanomolar inhibitor of P. falciparum asexual blood-stage growth with improved solubility and microsomal stability and reduced hERG binding. The build/couple/pair (B/C/P) synthet ...[more]