Literature DB >> 22408719

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

Erika E Englund1, Susanne Neumann, Elena Eliseeva, Joshua G McCoy, Steven Titus, Wei Zheng, Noel Southall, Paul Shin, William Leister, Craig J Thomas, James Inglese, Christopher P Austin, Marvin C Gershengorn, Wenwei Huang.   

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.

Entities:  

Year:  2011        PMID： 22408719      PMCID： PMC3293179          DOI： 10.1039/C1MD00145K

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  26 in total

1.  The first orally active low molecular weight agonists for the LH receptor: thienopyr(im)idines with therapeutic potential for ovulation induction.

Authors:  N C R van Straten; G G Schoonus-Gerritsma; R G van Someren; J Draaijer; A E P Adang; C M Timmers; R G J M Hanssen; C A A van Boeckel
Journal:  Chembiochem       Date:  2002-10-04       Impact factor: 3.164

2.  TSH receptor monoclonal antibodies with agonist, antagonist, and inverse agonist activities.

Authors:  Jane Sanders; Ricardo Núñez Miguel; Jadwiga Furmaniak; Bernard Rees Smith
Journal:  Methods Enzymol       Date:  2010       Impact factor: 1.600

Review 3.  The genetics of the thyroid stimulating hormone receptor: history and relevance.

Authors:  Terry F Davies; Xiaoming Yin; Rauf Latif
Journal:  Thyroid       Date:  2010-07       Impact factor: 6.568

4.  Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.

Authors:  Susanna Moore; Holger Jaeschke; Gunnar Kleinau; Susanne Neumann; Stefano Costanzi; Jian-kang Jiang; John Childress; Bruce M Raaka; Anny Colson; Ralf Paschke; Gerd Krause; Craig J Thomas; Marvin C Gershengorn
Journal:  J Med Chem       Date:  2006-06-29       Impact factor: 7.446

5.  Thyrotropin receptor expression in adrenal, kidney, and thymus.

Authors:  C M Dutton; W Joba; C Spitzweg; A E Heufelder; R S Bahn
Journal:  Thyroid       Date:  1997-12       Impact factor: 6.568

6.  Thyroid-stimulating hormone receptor and thyroid hormone receptors are involved in human endometrial physiology.

Authors:  Lusine Aghajanova; Anneli Stavreus-Evers; Maria Lindeberg; Britt-Marie Landgren; Lottie Skjöldebrand Sparre; Outi Hovatta
Journal:  Fertil Steril       Date:  2010-08-05       Impact factor: 7.329

Review 7.  Thyrotropin and homologous glycoprotein hormone receptors: structural and functional aspects of extracellular signaling mechanisms.

Authors:  Gunnar Kleinau; Gerd Krause
Journal:  Endocr Rev       Date:  2009-01-27       Impact factor: 19.871

Review 8.  A molecular dissection of the glycoprotein hormone receptors.

Authors:  Gilbert Vassart; Leonardo Pardo; Sabine Costagliola
Journal:  Trends Biochem Sci       Date:  2004-03       Impact factor: 13.807

9.  A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).

Authors:  Holger Jäschke; Susanne Neumann; Susanna Moore; Craig J Thomas; Anny-Odile Colson; Stefano Costanzi; Gunnar Kleinau; Jian-Kang Jiang; Ralf Paschke; Bruce M Raaka; Gerd Krause; Marvin C Gershengorn
Journal:  J Biol Chem       Date:  2006-02-16       Impact factor: 5.157

10.  Metolazone in treatment of severe refractory congestive cardiac failure.

Authors:  A Kiyingi; M J Field; C C Pawsey; J Yiannikas; J R Lawrence; W J Arter
Journal:  Lancet       Date:  1990-01-06       Impact factor: 79.321
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  3 in total

1.  Enantioselective Synthesis of Fluoro-Dihydroquinazolones and -Benzooxazinones by Fluorination-Initiated Asymmetric Cyclization Reactions.

Authors:  Kenichi Hiramatsu; Takashi Honjo; Vivek Rauniyar; F Dean Toste
Journal:  ACS Catal       Date:  2015-12-04       Impact factor: 13.084

Review 2.  2,3-Dihydroquinazolin-4(1H)-one as a privileged scaffold in drug design.

Authors:  Mariateresa Badolato; Francesca Aiello; Nouri Neamati
Journal:  RSC Adv       Date:  2018-06-07       Impact factor: 4.036

3.  Synthesis of a Pyrrolo[1,2-a]quinazoline-1,5-dione Derivative by Mechanochemical Double Cyclocondensation Cascade.

Authors:  Vanessza Judit Kolcsár; György Szőllősi
Journal:  Molecules       Date:  2022-09-02       Impact factor: 4.927
  3 in total

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