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Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: par

Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: par

  1. Anonymous
    Bioorg Med Chem Lett. 2008 Feb 1;18(3):1091-5. Epub 2007 Dec 8.
    Woltering TJ, Adam G, Wichmann J, Goetschi E, Kew JN, Knoflach F, Mutel V, Gatti S.

    Abstract
    A series of 1,3-dihydro-benzo[1,4]diazepin-2-one derivatives was evaluated as non-competitive mGluR2/3 antagonists. Replacement of a cyano group by a five-membered heterocycle produced compounds inhibiting the binding of [(3)H]-LY354740 to rat mGluR2 with low nanomolar affinity and consistent functional effect at both mGluR2 and mGluR3. Further modification to improve the physicochemical properties led eventually to compounds with the ability to reverse LY354740-mediated inhibition of field excitatory postsynaptic potentials in the rat dentate gyrus.

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