Outline
DOI: 10.1021/acsmedchemlett.6c00537 ISSN: 1948-5875
Novel Triazolopyrimidine Analogs as Glucosylceramide Synthase Inhibitors
Yinlong Li, Luke Rasmituth, Steven H. LiangAbstract
This highlight presents a recent patent disclosing a series of triazolopyrimidine-derived analogs as inhibitors of glucosylceramide synthase (GCS). The disclosed compounds exhibit potent GCS inhibition, with selected analogs showing picomolar to subnanomolar EC50 values, and are claimed for use in treating diseases and disorders associated with GCS activity. Optimized analogs also demonstrate brain penetration, microsomal stability, and favorable plasma protein binding profiles.
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