An H, Haly B D, Cook P D
Isis Pharmaceuticals, Inc., Carlsbad, CA 92008, USA.
Bioorg Med Chem Lett. 1998 Sep 8;8(17):2345-50. doi: 10.1016/s0960-894x(98)00424-7.
Four novel unsymmetric piperazinyl polyazacyclophane scaffolds 1-4 were synthesized in high yields by an efficient cyclization strategy. Twenty-six libraries 12-37 (total 16,000 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.
通过一种高效的环化策略，以高产率合成了四种新型不对称哌嗪基聚氮杂环番支架1-4。采用溶液相组合方法，由1-4和38种官能团生成了26个文库12-37（共16000种化合物）。发现了强效的抗菌活性以及HIV-1反式激活因子/转录激活反应元件（tat/TAR）蛋白-RNA干扰活性。
