Work

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

Year: 2011

Type: article

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.

Source: MedChemComm

DOI: 10.1039/c1md00145k

Authors: 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

Institutions: National Institutes of Health, National Institute of Diabetes and Digestive and Kidney Diseases

Language: English

Topic: Quinazolinone synthesis and applications

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Institutes of Health, National Human Genome Research Institute

Award: NIH Chemical Genomics Center

OpenAlex ID: W2134983008

FWCI: 0.151

Cites: 26

Cited by: 11

Related to: 10