Ontology highlight
ABSTRACT:
SUBMITTER: Mueller R
PROVIDER: S-EPMC7114883 | biostudies-literature | 2020 Mar
REPOSITORIES: biostudies-literature
Mueller Rudolf R Reddy Virsinha V Nchinda Aloysius T AT Mebrahtu Fanuel F Taylor Dale D Lawrence Nina N Tanner Lloyd L Barnabe Marine M Eyermann Charles J CJ Zou Bin B Kondreddi Ravinder R RR Lakshminarayana Suresh B SB Rottmann Matthias M Street Leslie J LJ Chibale Kelly K
ACS omega 20200317 12
A phenotypic whole cell high-throughput screen against the asexual blood and liver stages of the malaria parasite identified a benzimidazole chemical series. Among the hits were the antiemetic benzimidazole drug Lerisetron <b>1</b> (IC<sub>50</sub> NF54 = 0.81 μM) and its methyl-substituted analogue <b>2</b> (IC<sub>50</sub> NF54 = 0.098 μM). A medicinal chemistry hit to lead effort led to the identification of chloro-substituted analogue <b>3</b> with high potency against the drug-sensitive NF5 ...[more]