期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 18, 页码 5091-5096出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.07.029
关键词
Glutamate; GPCR; mGlu(1); Allosteric modulator; CNS; Octahydropyrrolo[3,4-c]pyrrole
资金
- Seaside Therapeutics [VUMC36176]
Development of SAR in an octahydropyrrolo[3,4-c]pyrrole series of negative allosteric modulators of mGlu(1) using a functional cell-based assay is described in this Letter. The octahydropyrrolo[3,4-c]pyrrole scaffold was chosen as an isosteric replacement for the piperazine ring found in the initial hit compound. Characterization of selected compounds in protein binding assays was used to identify the most promising analogs, which were then profiled in P450 inhibition assays in order to further assess the potential for drug-likeness within this series of compounds. (C) 2013 Elsevier Ltd. All rights reserved.
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