title: The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.
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.
authors.affiliation: NIH Chemical Genomics Center, 9800 Medical Center Drive, Building B, Bethesda MD, 20892-3371.
authors.forename: Erika E
authors.initials: EE
authors.lastname: Englund
authors.forename: Susanne
authors.initials: S
authors.lastname: Neumann
authors.forename: Elena
authors.initials: E
authors.lastname: Eliseeva
authors.forename: Joshua G
authors.initials: JG
authors.lastname: McCoy
authors.forename: Steven
authors.initials: S
authors.lastname: Titus
authors.forename: Wei
authors.initials: W
authors.lastname: Zheng
authors.forename: Noel
authors.initials: N
authors.lastname: Southall
authors.forename: Paul
authors.initials: P
authors.lastname: Shin
authors.forename: William
authors.initials: W
authors.lastname: Leister
authors.forename: Craig J
authors.initials: CJ
authors.lastname: Thomas
authors.forename: James
authors.initials: J
authors.lastname: Inglese
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Austin
authors.forename: Marvin C
authors.initials: MC
authors.lastname: Gershengorn
authors.forename: Wenwei
authors.initials: W
authors.lastname: Huang