The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.

Medicinal Chemistry


We herein describe the rapid synthesis of a diverse set of dihydroquinazolin-4-ones and quinazolin-4-ones, their biological evaluation as thyroid stimulating hormone receptor (TSHR) agonists, and SAR analysis. Among the compounds screened, 8b was 60-fold more potent than the hit compound 1a, which was identified from a high throughput screen of over 73,000 compounds.


Englund, Erika E; Neumann, Susanne; Eliseeva, Elena; McCoy, Joshua G; Titus, Steven; Zheng, Wei; Southall, Noel; Shin, Paul; Leister, William; Thomas, Craig; Inglese, James; Austin, Christopher; Gershengorn, Marvin C; Huang, Wenwei;

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