Synthesis and receptor binding studies of halogenated N, N-dialkylel-(2-phenyl-1H-indol-3-yl) glyoxylamides to visualize peripheral benzodiazepine receptors with …
I Bennacef, CN Haile, A Schmidt, AO Koren…
Index: Bennacef, Idriss; Haile, Colin N.; Schmidt, Anne; Koren, Andrei O.; Seibyl, John P.; Staley, Julie K.; Bois, Frederic; Baldwin, Ronald M.; Tamagnan, Gilles Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 22 p. 7582 - 7591
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Citation Number: 16
Abstract
A library of halogenated 2-arylindolyl-3-oxocarboxamides was prepared to develop radioligands to visualize cerebral PBR by SPECT and PET imaging. In vitro evaluation showed that most of the synthesized compounds were selective, high-affinity PBR ligands with adequate lipophilicity (logD7. 4 in the range of 1.6–2.4). The iodinated derivative 11 (Ki= 2.6 nM) and the fluorinated analog 26 (Ki= 6.2 nM) displayed higher affinity than ...
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