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 journalArticle

4 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 Sep 2019

Fingerprint Dive into the research topics of 'First nondiscriminating translocator protein ligands produced from a carbazole scaffold'. Together they form a unique fingerprint.

  • Cite this