New piperazinyl polyazacyclophane scaffolds, libraries and biological activities

被引:16
作者
An, HY [1 ]
Haly, BD [1 ]
Cook, PD [1 ]
机构
[1] ISIS Pharmaceut, Carlsbad, CA 92008 USA
关键词
D O I
10.1016/S0960-894X(98)00424-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2345 / 2350
页数:6
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