Xu Yu-Wen, Zhao Gui-Sen, Shin Cha-Gyun, Zang Heng-Chang, Lee Chong-Kyo, Lee Yong Sup
College of Pharmacy, Shandong University, PO Box 111, 44# Wenhuaxi Road, Ji'nan 250012, Shandong Province, PR China.
Bioorg Med Chem. 2003 Aug 15;11(17):3589-93. doi: 10.1016/s0968-0896(03)00372-9.
HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors. Among these compounds, we found that HIV integrase inhibitory activities of compounds III-3 and III-4 were more potent than L-chicoric acid (IC(50)=11.8 microg/mL) and others were comparable to L-chicoric acid. Furthermore, the structure-activity relationships of these compounds were studied. The information gathered from this paper will be useful in the development and design of HIV-1 integrase inhibitors in the future.
HIV-1整合酶（IN）是逆转录病毒复制所必需的酶，也是抗艾滋病药物设计的合理靶点。在本研究中，我们设计、合成并测试了一系列咖啡酰萘磺酰胺衍生物作为HIV整合酶抑制剂。在这些化合物中，我们发现化合物III-3和III-4对HIV整合酶的抑制活性比L-菊苣酸（IC(50)=11.8微克/毫升）更强，其他化合物与L-菊苣酸相当。此外，还研究了这些化合物的构效关系。从本文收集的信息将有助于未来HIV-1整合酶抑制剂的开发和设计。
