… and characterization of 8-ethynyl-1, 3-dihydro-benzo [b][1, 4] diazepin-2-one derivatives: Part 2. New potent non-competitive metabotropic glutamate receptor 2/3 …

TJ Woltering, G Adam, J Wichmann, E Goetschi…

Index: Woltering, Thomas J.; Adam, Geo; Wichmann, Juergen; Goetschi, Erwin; Kew, James N.C.; Knoflach, Frederic; Mutel, Vincent; Gatti, Silvia Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1091 - 1095

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Citation Number: 17

Abstract

A series of 1, 3-dihydro-benzo [b][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 [3H]-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 ...