Three-component, one-pot synthesis of novel 2,4-substituted 5-azolylthiopyrimidine library for screening against anti-influenza virus A

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• 作者：Gang Cheng ; Shukun Li ; Jingya Li ; Youhong Hu
• 关键词：One-pot synthesis ; Michael-addition ; Condensation ; 5-Azolylthiopyridines ; Heterocycle libraries ; Anti-influenza
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 February 2008
• 年：2008
• 卷：18
• 期：3
• 页码：1177-1180
• 全文大小：118 K

文摘

A novel one-pot synthesis of 2,4-substituted 5-azolylthiopyrimidines is achieved by sequential Michael-addition of 3-iodochromones with mercaptoazole (or mercaptotriazoles) and then condensation with a variety of amidines. Compound A₁B₆C₁ exhibits a potent anti-influenza virus A activity with an IC₅₀ value of 21.56 mg/mL and SI value of 9.