First nondiscriminating translocator protein ligands produced from a carbazole scaffold

Hei Wun Alison Cheng, Renee Sokias, Eryn L. Werry, Lars M. Ittner, Tristan A. Reekie, Jonathan Du, Quanqing Gao, David E. Hibbs, Michael Kassiou*

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    13 Citations (Scopus)

    Abstract

    Development of neuroinflammation agents targeting the translocator protein (TSPO) has been hindered by a common single nucleotide polymorphism (A147T) at which TSPO ligands commonly lose affinity. To this end, carbazole acetamide scaffolds were synthesized and structure activity relationships elaborated to explore the requirements for high-affinity binding to both TSPO wild type (WT) and the polymorphic TSPO A147T. This study reports high binding affinity and nondiscriminating TSPO ligands.

    Original languageEnglish
    Pages (from-to)8235-8248
    Number of pages14
    JournalJournal of Medicinal Chemistry
    Volume62
    Issue number17
    DOIs
    Publication statusPublished - 12 Sept 2019

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