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. Author manuscript; available in PMC: 2021 Nov 15.
Published in final edited form as: Bioorg Med Chem. 2020 Sep 1;28(22):115734. doi: 10.1016/j.bmc.2020.115734

Scheme 1.

Scheme 1.

GSM B-ring optimization. Aminothiazole 3 (NGP-555) represents the initial lead compound for efforts to discover a potent GSM with improved ADMET properties. Tetrahydroindazole D-ring analog 4 was developed with the aim of improving critical properties of compound 3, including solubility. The rings are labeled A-D for clarity.