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Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand.

Abstract：

:Optimization of the pharmacokinetic properties for a series of benzoxazolone derivatives led to the identification of 9b, which showed anxiolytic effect in a rat model. However, 9b, like known benzodiazepines, induced motor impairment. Investigation into the cause of this unexpected side effect and management of 9b off-target binding affinity led to the identification of 10d, which showed oral anxiolytic effect in the rat model with improved safety profile.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Fukaya T,Ishiyama T,Baba S,Masumoto S

doi

10.1021/jm401325r

subject

Has Abstract

pub_date

2013-10-24 00:00:00

pages

8191-5

issue

20

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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