| Title | The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists. |
| Publication Type | Journal Article |
| Year of Publication | 2011 |
| Authors | Englund 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 |
| Journal | Medchemcomm |
| Volume | 2 |
| Issue | 10 |
| Pagination | 1016-1020 |
| Date Published | 2011 Oct |
| ISSN | 2040-2503 |
| 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. |
| DOI | 10.1039/C1MD00145K |
| Alternate Journal | Medchemcomm |
| PubMed ID | 22408719 |
| PubMed Central ID | PMC3293179 |
| Grant List | Z01 HG200319-04 / HG / NHGRI NIH HHS / United States |