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Peripherally restricted CB1 receptor inverse agonists hold potential as useful therapeutics to treat obesity and related metabolic diseases without causing undesired CNS-mediated adverse effects. We identified a series of tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and highly peripherally selective CB1 receptor inverse agonists. This discovery was achieved by introducing polar functional groups into the molecule, which increase the topological polar surface area and reduce its brain-penetrating ability. Copyright © 2016 Elsevier Ltd. All rights reserved.


Bin Zhu, Jay M Matthews, Mingde Xia, Shawn Black, Cailin Chen, Cuifen Hou, Yin Liang, Yuting Tang, Mark J Macielag. Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists. Bioorganic & medicinal chemistry letters. 2016 Nov 15;26(22):5597-5601

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PMID: 27671499

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