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

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.

SUBMITTER: Englund EE

PROVIDER: S-EPMC3293179 | biostudies-literature | 2011 Oct

REPOSITORIES: biostudies-literature

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

Englund Erika E EE Neumann Susanne S Eliseeva Elena E McCoy Joshua G JG Titus Steven S Zheng Wei W Southall Noel N Shin Paul P Leister William W Thomas Craig J CJ Inglese James J Austin Christopher P CP Gershengorn Marvin C MC Huang Wenwei W

MedChemComm 20111001 10

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. ...[more]

PMID: 22408719

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