25 Feb 2021
Journal of Medicinal Chemistry
PMID: 33573376
Doi: 10.1021/acs.jmedchem.1c00034

Photo: gerasimov_foto_174/Shutterstock.com
A novel diazaspiro[3.4]octane series was identified from a whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp-rich scaffold provided an attractive starting point for a hit-to-lead medicinal chemistry optimization and biological profiling program. Structure-activity-relationship studies led to the identification of compounds that showed low nanomolar asexual blood-stage activity.
To view the full article please visit the ACS Publications website.