The synthesis and evaluation of dihydroquinazolin-4-ones and quinazolin-4-ones as thyroid stimulating hormone receptor agonists

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

doi:10.1039/C1MD00145K

The synthesis and evaluation of dihydroquinazolin-4-ones and quinazolin-4-ones as thyroid stimulating hormone receptor agonists†

Erika E. Englund,^a Susanne Neumann,^b Elena Eliseeva,^b Joshua G. McCoy,^a Steven Titus,^a Wei Zheng,^a Noel Southall,^a Paul Shinn,^a William Leister,^a Craig J. Thomas,^a James Inglese,^a Christopher P. Austin,^a Marvin C. Gershengorn^b and Wenwei Huang*^a

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^a NIH Chemical Genomics Center, 9800 Medical Center Drive, Building B, Bethesda, MD, USA

^b National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), Bethesda, MD, USA

Abstract

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.

MedChemComm

The synthesis and evaluation of dihydroquinazolin-4-ones and quinazolin-4-ones as thyroid stimulating hormone receptor agonists†

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The synthesis and evaluation of dihydroquinazolin-4-ones and quinazolin-4-ones as thyroid stimulating hormone receptor agonists

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