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

…, T Kodo, T Ishiyama, H Kakuyama, H Nishikawa…

Index: Fukaya, Takayuki; Kodo, Toru; Ishiyama, Takeo; Kakuyama, Hiroyoshi; Nishikawa, Hiroyuki; Baba, Satoko; Masumoto, Shuji Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 18 p. 5568 - 5582

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Citation Number: 7

Abstract

Selective 18kDa 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 ...