4.7 Article

Design, synthesis and anxiolytic-like activity of 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 13, Pages 3368-3378

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.04.049

Keywords

Anxiolytic activity; Elevated plus maze test; Open field test; PK11195; Pyrrolo[1,2-a]pyrazines; TSPO; Vinyl azides

Funding

  1. Basic Research Program of the Presidium of the Russian Academy of Sciences

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A series of 1-arylpyrrolo[1,2-a] pyrazine-3-carboxamides were designed and synthesized as 18 kDa translocator protein (TSPO) ligands. Anxiolytic-like activity of compounds was evaluated in the open field test and elevated plus maze test. Compounds 1a and 1b demonstrated high anxiolytic-like effect in the dose range of 0.1-1.0 mg/kg comparable with that of diazepam. The involvement of TSPO receptor in the mechanism of anxiolytic-like activity of new compounds was proved by antagonism of the most active compound 1a with TSPO selective inhibitor PK11195. In vitro binding studies demonstrated high TSPO affinities for compounds 1a and 1b. (C) 2015 Elsevier Ltd. All rights reserved.

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