Title of article :
Design, synthesis and structure–affinity relationships of aryloxyanilide derivatives as novel peripheral benzodiazepine receptor ligands Original Research Article
Author/Authors :
Taketoshi Okubo، نويسنده , , Ryoko Yoshikawa، نويسنده , , Shigeyuki Chaki، نويسنده , , Shigeru Okuyama، نويسنده , , Atsuro Nakazato، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Pages :
16
From page :
423
To page :
438
Abstract :
Since the peripheral benzodiazepine receptor (PBR) has been primarily found as a high-affinity binding site for diazepam in rat kidney, numerous studies of it have been performed. However, the physiological role and functions of PBR have not been fully elucidated. Currently, we presented the pharmacological profile of two high and selective PBR ligands, N-(2,5-dimethoxybenzyl)-N-(4-fluoro-2-phenoxyphenyl)acetamide (7-096, DAA1106) (PBR: IC50=0.28 nM) and N-(4-chloro-2-phenoxyphenyl)-N-(2-isopropoxybenzyl)acetamide (7-099, DAA1097) (PBR: IC50=0.92 nM). The compounds are aryloxyanilide derivatives, and identified with known PBR ligands such as benzodiazepine (1, Ro5-4864), isoquinoline (2, PK11195), imidazopyridine (3, Alpidem), and indole (5, FGIN-1-27) derivatives. The aryloxyanilide derivatives, which have been derived by opening the diazepine ring of 1, are a novel class as PBR ligands and have exhibited high and selective affinity for peripheral benzodiazepine receptors (PBRs). These novel derivatives would be useful for exploring the functions of PBR. In this paper, the design, synthesis and structure–affinity relationships of aryloxyanilide derivatives are described.
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2004
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1302876
Link To Document :
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