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

Gang Cheng; Shukun Li; Jingya Li; Youhong Hu

doi:10.1016/j.bmcl.2007.11.117

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. Epub 2007 Dec 4.

Authors

Gang Cheng¹, Shukun Li, Jingya Li, Youhong Hu

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antiviral Agents / chemical synthesis*
Antiviral Agents / chemistry
Antiviral Agents / pharmacology*
Combinatorial Chemistry Techniques*
Influenza A virus / drug effects*
Molecular Structure
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology*

Substances

Antiviral Agents
Pyrimidines