Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein

HIV-1 capsid protein (CA) plays important roles in the viral replication cycle. A number of acylhydrazone derivatives that act as inhibitors of HIV-1 CA assembly, were designed and synthesized. The synthesized compounds were tested for their antiviral activities and cytotoxicities using CEM cells. Some derivatives also were assayed for their ability to inhibit HIV-1 CA assembly in vitro. Among them, compounds 14f and 14i display the most promising potency with EC50 values of 0.21 and 0.17 μΜ, respectively.

Graphical abstractA variety of novel acylhydrazone derivatives were synthesized and tested for their antiviral activities as inhibitors of HIV-1 capsid assembly. Compounds 14f and 14i could inhibit HIV-1 capsid assembly strongly and displayed the most promising potency (EC50 = 0.21 and 0.17 μΜ).Figure optionsDownload full-size imageDownload as PowerPoint slide