Department of Anesthesiology

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

TitleThe Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.
Publication TypeJournal Article
Year of Publication2011
AuthorsEnglund EE, Neumann S, Eliseeva E, McCoy JG, Titus S, Zheng W, Southall N, Shin P, Leister W, Thomas CJ, Inglese J, Austin CP, Gershengorn MC, Huang W
JournalMedchemcomm
Volume2
Issue10
Pagination1016-1020
Date Published2011 Oct
ISSN2040-2503
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.

DOI10.1039/C1MD00145K
Alternate JournalMedchemcomm
PubMed ID22408719
PubMed Central IDPMC3293179
Grant ListZ01 HG200319-04 / HG / NHGRI NIH HHS / United States