New piperazinyl polyazacyclophane scaffolds, libraries and biological activities

Four novel unsymmetric piperazinyl polyazacyclophane scaffolds 1–4 were synthesized in high yields by an efficient cyclization strategy. Twenty-six libraries 12–37 (total 16000 compounds) were generated by a solution-phase combinatorial approach from 1–4 and thirty-eight functional groups. Potent antibacterial and HIV-1 tat/TAR protein-RNA disrupting activities were discovered.