Ontology highlight
ABSTRACT:
SUBMITTER: Ding S
PROVIDER: S-EPMC7422479 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Ding Sha S Fike Katherine R KR Klemba Michael M Carlier Paul R PR
Bioorganic & medicinal chemistry letters 20200624 17
Antimalarial candidates possessing novel mechanisms of action are needed to control drug resistant Plasmodium falciparum. We were drawn to Malaria Box compound 1 (MMV665831) by virtue of its excellent in vitro potency, and twelve analogs were prepared to probe its structure-activity relationship. Modulation of the diethyl amino group was fruitful, producing compound 25, which was twice as potent as 1 against cultured parasites. Efforts were made to modify the phenolic Mannich base functionality ...[more]