Three-component, one-pot synthesis of novel 2,4-substituted 5-azolylthiopyrimidine library for screening against anti-influenza virus A.
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.
Cheng
Gang
G
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.
Li
Shukun
S
Li
Jingya
J
Hu
Youhong
Y
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D009980:Influenza A virus / Q000187:drug effects*; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000998:Antiviral Agents; D011743:Pyrimidines