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

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

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):1177-80. doi: 10.1016/j.bmcl.2007.11.117.
Gang Cheng 1,  Shukun Li,  Jingya Li,  Youhong Hu
Affiliations

Affiliation

  • 1 Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.
PMID: 18160286 DOI: 10.1016/j.bmcl.2007.11.117
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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