A novel class of potent influenza virus inhibitors: polysubstituted acylthiourea and its fused heterocycle derivatives.
A series of polysubstituted and fused heterocycle derivatives of acylthiourea was prepared and the biological activity against influenza virus was evaluated. Of the analogues that demonstrated IC(50)s<0.1 microM, acylthiourea derivatives 16 and 50 were further investigated as candidates with the most potential for future development. The SAR of these compounds are discussed and they represent a novel class of highly potent and selective inhibitors of influenza virus.
Sun
Chuanwen
C
Bio-X Life Science Research Center, Department of Life Science and Technology, Shanghai Jiaotong University, Shanghai 200030, China. sunwillin@sjtu.edu.cn
Huang
Hai
H
Feng
Meiqing
M
Shi
Xunlong
X
Zhang
Xiaodong
X
Zhou
Pei
P
D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002460:Cell Line; D004285:Dogs; D006801:Humans; D007251:Influenza, Human / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D009975:Orthomyxoviridae / Q000378:metabolism*; D011741:Pyrimidine Nucleosides / Q000737:chemistry; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000737:chemistry
D000998:Antiviral Agents; D011741:Pyrimidine Nucleosides; D013890:Thiourea