Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors.
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.
Xu
Yu-Wen
YW
College of Pharmacy, Shandong University, PO Box 111, 44# Wenhuaxi Road, Ji'nan 250012, Shandong Province, PR China.
Zhao
Gui-Sen
GS
Shin
Cha-Gyun
CG
Zang
Heng-Chang
HC
Lee
Chong-Kyo
CK
Lee
Yong Sup
YS
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D019427:HIV Integrase / Q000737:chemistry / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D019380:Anti-HIV Agents; D019428:HIV Integrase Inhibitors; D013449:Sulfonamides; C051353:naphthalenesulfonamide; D019427:HIV Integrase