Synthesis and biological activities on batzelladine derivatives

Structure-activity relationship studies on batzelladines A and D were examined. Seven batzelladine derivatives, including 24-epi-batzelladine A (3) and 7-epi-batzelladine D (4), were synthesized. The inhibitory activity of these derivatives on binding of gp120 with CD4 was evaluated by the use of ELISA-based assay method. For the potent biological activities of batzelladines, tricyclic guanidine moiety, a common structure of batzelladine A and D, and side chain bearing guanidine functional group were found to be mandatory.