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Issue 10, 2011
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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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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.

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

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Publication details

The article was received on 09 Jun 2011, accepted on 27 Jul 2011 and first published on 30 Aug 2011


Article type: Concise Article
DOI: 10.1039/C1MD00145K
Med. Chem. Commun., 2011,2, 1016-1020

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

    E. E. Englund, S. Neumann, E. Eliseeva, J. G. McCoy, S. Titus, W. Zheng, N. Southall, P. Shinn, W. Leister, C. J. Thomas, J. Inglese, C. P. Austin, M. C. Gershengorn and W. Huang, Med. Chem. Commun., 2011, 2, 1016
    DOI: 10.1039/C1MD00145K

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