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 IC50s < 0.1 μM, 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.

Graphical abstractA series of polysubstituted and fused heterocycle derivatives of acylthiourea was prepared and shown to be a novel class of highly potent and selective inhibitors of influenza virus. Derivatives 16 and 50 were further investigated as potential candidates for future development.Figure optionsDownload full-size imageDownload as PowerPoint slide