Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester.
A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3'-end processing and the strand transfer. Their key structure-activity relationship was also discussed.
Wang
Peng
P
School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province 250012, PR China.
Liu
Chuan
C
Sanches
Tino
T
Zhong
Yuan
Y
Liu
Bo
B
Xiong
Junlong
J
Neamati
Nouri
N
Zhao
Guisen
G
D002109:Caffeic Acids / Q000737:chemistry*; D015195:Drug Design; D019427:HIV Integrase / Q000737:chemistry* / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009584:Nitrogen / Q000737:chemistry; D010626:Phenylethyl Alcohol / Q000031:analogs & derivatives* / Q000737:chemistry; D013329:Structure-Activity Relationship
D002109:Caffeic Acids; D019428:HIV Integrase Inhibitors; D019427:HIV Integrase; C055494:caffeic acid phenethyl ester; D010626:Phenylethyl Alcohol; D009584:Nitrogen; C514801:p31 integrase protein, Human immunodeficiency virus 1