Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists
Year: 2010
Type: article
Abstract: A novel series of quinazolinone T-type calcium channel antagonists have been prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 by modifications of the 3- and 4-positions of the quinazolinone ring afforded potent and selective antagonists that displayed in vivo central nervous system efficacy in epilepsy and tremor models, as well as significant effects on rat active wake as measured by electrocorticogram.
Source: ACS Medicinal Chemistry Letters
DOI: 10.1021/ml100004r
Authors: James C. Barrow, Kenneth E. Rittle, Thomas S. Reger, Zhi-Qiang Yang, Phung Bondiskey, Georgia B. McGaughey, Mark G. Bock, George D. Hartman, Cuyue Tang, Jeanine Ballard, Yuhsin Kuo, Thomayant Prueksaritanont, Cindy E. Nuss, Scott M. Doran, Steven V. Fox, Susan L. Garson, Richard L. Kraus, Yuxing Li, Michael J. Marino, Valerie Kuzmick Graufelds, Victor N. Uebele, John J. Renger
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W2049829240