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
  • 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.