Aminophenoxazinones as Inhibitors of Indoleamine 2,3-Dioxygenase (IDO). Synthesis of Exfoliazone and Chandrananimycin A

作者:Pasceri Raffaele; Siegel David; Ross David*; Moody Christopher J
来源:Journal of Medicinal Chemistry, 2013, 56(8): 3310-3317.
DOI:10.1021/jm400049z

摘要

A range of 2-aminophenoxazin-3-ones has been prepared by oxidative cyclocondensation of 2-aminophenols, including the natural products exfoliazone and chandrananimycin A, both synthesized for the first time. The compounds were evaluated for their ability to inhibit indoleamine 2,3-dioxygenase. Compounds containing additional electron-withdrawing carboxylate groups, such as cinnabarinic acid, showed modest inhibitory activity with a dose response.

  • 出版日期2013-4-25