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.

A 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 as PowerPoint slide