We report the synthesis and the affinity data at both the peripheral (PBR) and the central benzodiazepine receptors of a series of N,N-dialkyl-2-phenylindol-3-ylglyoxylamide derivatives III, designed as conformationally constrained analogues of 2-phenylindole-3-acetamides II such as FGIN-1-27. Most of the new compounds showed a high specificity and affinity for PBR, with K i in the nanomolar to subnanomolar range. The most potent ligands (4-7, 9, 13-27) stimulated steroid biosynthesis in rat C6 glioma cells with a potency similar to or higher than that of classical ligands. The SARs of this new class of compounds are discussed.
|Autori:||G. PRIMOFIORE; DA SETTIMO PASSETTI F; S. TALIANI; F. SIMORINI; M.P. PATRIZI; E. NOVELLINO; G. GRECO; E. ABIGNENTE; B. COSTA; B. CHELLI; C. MARTINI|
|Titolo:||N,N-Dialkyl-2-phenylindol-3- ylglyoxylamides. A New Class of Potent and Selective Ligands at the Peripheral Benzodiazepine Receptor|
|Anno del prodotto:||2004|
|Digital Object Identifier (DOI):||10.1021/jm030973k|
|Appare nelle tipologie:||1.1 Articolo in rivista|