Bioorganic & medicinal chemistry

Synthesis and evaluation of a new series of substituted acyl (thio) urea and thiadiazolo [2, 3-a] pyrimidine derivatives as potent inhibitors of influenza virus …

C Sun, X Zhang, H Huang, P Zhou

Index: Sun, Chuanwen; Zhang, Xiaodong; Huang, Hai; Zhou, Pei Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 24 p. 8574 - 8581

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Citation Number: 53

Abstract

A series of substituted acyl (thio) urea and 2H-1, 2, 4-thiadiazolo [2, 3-a] pyrimidine derivatives were prepared and both of their cell culture and enzymatic activity toward influenza virus were tested. Their in vitro neuraminidase inhibitory activities were in good agreement with the corresponding activities in cultured cells and they were evaluated as potent neuraminidase inhibitors. Of the analogues that demonstrated IC50s< 0.1 μM, 16 ...