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

Bioorganic & Medicinal Chemistry Letters
2008.0

Abstract

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 A(1)B(6)C(1) exhibits a potent anti-influenza virus A activity with an IC(50) value of 21.56 mg/mL and SI value of 9.

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