Ontology highlight
ABSTRACT:
SUBMITTER: Comer E
PROVIDER: S-EPMC4207553 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
Comer Eamon E Beaudoin Jennifer A JA Kato Nobutaka N Fitzgerald Mark E ME Heidebrecht Richard W RW Lee Maurice duPont Md Masi Daniela D Mercier Marion M Mulrooney Carol C Muncipinto Giovanni G Rowley Ann A Crespo-Llado Keila K Serrano Adelfa E AE Lukens Amanda K AK Wiegand Roger C RC Wirth Dyann F DF Palmer Michelle A MA Foley Michael A MA Munoz Benito B Scherer Christina A CA Duvall Jeremy R JR Schreiber Stuart L SL
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]