Discovery and expanded SAR of 4,4-disubs
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Kelly-Ann S. Schlegel; Zhi-Qiang Yang; Thomas S. Reger; Youheng Shu; Rowena Cube
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Article
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2010
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Elsevier Science
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English
โ 615 KB
The discovery and synthesis of 4,4-disubstituted quinazolinones as T-type calcium channel antagonists is reported. Based on lead compounds 2 and 3, a focused SAR campaign driven by the optimization of potency, metabolic stability, and pharmacokinetic profile identified 45 as a potent T-type Ca(2+) c