Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators

Cannabinoid 1 receptor (CB1R) allosteric ligands hold a far-reaching therapeutic promise. We report the 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 exhi...

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Bibliographic Details
Published in:Journal of medicinal chemistry Vol. 63; no. 2; pp. 542 - 568
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: Journal Article
Language:English
Published: WASHINGTON Amer Chemical Soc 23.01.2020
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ISSN:0022-2623, 1520-4804, 1520-4804
Online Access:Get more information
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