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

Sumanta Garai, Pushkar M. Kulkarni, Peter C. Schaffer, Luciana M. Leo, Asher L. Brandt, Ayat Zagzoog, Tallan Black, Xiaoyan Lin, Dow P. Hurst, David R. Janero,

Journal of Medicinal Chemistry · 2019 · 60 citations · 41 references

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Abstract

), exhibited moderate ago-PAM potency and improved aqueous solubility with therapeutic reduction of intraocular pressure in murine glaucoma models. The SAR findings and the enhanced allosteric activity in this class of allosteric modulators were accounted for in our recently developed computational model for CB1R allosteric activation and positive allosteric modulation.

References

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