Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of CB1 Receptor Positive Allosteric Modulators

Cannabinoid 1 receptor (CB1R) allosteric ligands hold far-reaching therapeutic promise. We report application of fluoro- and nitrogen-walk approaches to enhance the drug-like properties of GAT211, a prototype CB1R allosteric agonist-positive allosteric modulator (ago-PAM). Several analogs exhibited...

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Udgivet i:J Med Chem
Main Authors: Garai, Sumanta, Kulkarni, Pushkar M., Schaffer, Peter C., Leo, Luciana M., Brandt, Asher L., Zagzoog, Ayat, Black, Tallan, Lin, Xiaoyan, Hurst, Dow P., Janero, David R., Abood, Mary E., Zimmowitch, Anaelle, Straiker, Alex, Pertwee, Roger G., Kelly, Melanie, Szczesniak, Anna-Maria, Denovan-Wright, Eileen M., Mackie, Ken, Hohmann, Andrea G., Reggio, Patricia H., Laprairie, Robert B., Thakur, Ganesh A.
Format: Artigo
Sprog:Inglês
Udgivet: 2020
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7077750/
https://ncbi.nlm.nih.gov/pubmed/31756109
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b01142
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