Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity |
| |
Authors: | Yu Shenghui Zhang Linna Yan Shifeng Wang Peng Sanchez Tino Christ Frauke Debyser Zeger Neamati Nouri Zhao Guisen |
| |
Institution: | Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University , Jinan, Shandong , PR China. |
| |
Abstract: | Four series of forty-five nitrogen-containing polyhydroxylated aromatics based on caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase (IN) inhibitors. Most of these compounds inhibited IN catalytic activities in low micromolar range. Among these new analogues, compounds 9e and 9f were the most potent IN inhibitors with IC(50) value of 0.7 μM against strand transfer reaction. Their key structure-activity relationships were also discussed. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|