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  • Title: N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
    Author: Primofiore G, Da Settimo F, Taliani S, Simorini F, Patrizi MP, Novellino E, Greco G, Abignente E, Costa B, Chelli B, Martini C.
    Journal: J Med Chem; 2004 Mar 25; 47(7):1852-5. PubMed ID: 15027878.
    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.
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