Referenced in: none

Automatically associated channels: Slo1

Title: Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands.

Authors: Takayuki Fukaya, Toru Kodo, Takeo Ishiyama, Hiroyoshi Kakuyama, Hiroyuki Nishikawa, Satoko Baba, Shuji Masumoto

Journal, date & volume: Bioorg. Med. Chem., 2012 Sep 15 , 20, 5568-82

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22884355

Abstract
Selective 18 kDa translocator protein (TSPO) ligands are expected to be therapeutic agents with a wide spectrum of action on psychiatric disorders and fewer side effects. We designed novel benzoxazolone derivatives and examined the structure-activity relationship (SAR) of a series of compounds with various substituents at the amide part and C-5 position. Although a number of the synthesized compounds showed high TSPO binding affinity, these compounds had poor drug-like properties. Further optimization of pharmacokinetic properties of these compounds led to discovery of compound 74, which exhibited anxiolytic effect in the rat Vogel conflict model.