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.

N, N-Dialkyl-2-phenylindol-3-ylglyoxylamides.A new class of potent and selective ligands at the Peripheral benzodiazepine receptor

DA SETTIMO PASSETTI, FEDERICO;TALIANI, SABRINA;SIMORINI, FRANCESCA;COSTA, BARBARA;MARTINI, CLAUDIA
2004

Abstract

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.
Primofiore, G; DA SETTIMO PASSETTI, Federico; Taliani, Sabrina; Simorini, Francesca; Patrizi, Mp; Novellino, E; Greco, G; Abignente, E; Costa, Barbara; Chelli, B; Martini, Claudia
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/86573
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