The Design And Synthesis Of Resdelabe

AIDS is an acquired immune deficiency syndrome, which is caused by retrovirus HIV. Since the first AIDS sufferer was reported in 1981, 70 million pepole have been infected with HIV in the world, and 20 million of them died. AIDS has become a main menace to human health. Anti-HIV drugs are divided into four groups on the basis of mechanism and they are nucleoside reverse transcriptase inhibitor (NRTIs), non-reverse transcriptase inhibitor (NNRTIs), protease inhibitors (PIs) and fusing inhibitor. On the other hand, because of the incessant variation of HIV, HIV is tolerance of widly-used medicines. Although effective drugs are used in treating HIV, which have declined dead ratio, the number of people infected with HIV is increasing sharply in recent years. It is the high time that we take effective measures to empolder new anti-HIV drugs. Generally speaking, HIV can destroy immunity system, which cause the human body to lose resistent ability against various pathogeny. And then various infections and tumours occurred, ultimately leading to death. The anti-HIV drugs are widely used at present, if we can empolder a new drug, which has functions of not only the antivirus activity but also improving human immunity, it can provide a new idea for AIDS treatment. In this study, we aim to link a natural immunocompetent compound to an anti-HIV compound. We expect that the new compound can enhance the ability of anti-variability. It has not only the effect of the antivirus activity but also improvement of humen immunity.Resdelabe,1-[3-[(1-methyl-ethyl)amino]-2-pyridinyl]-4-[[5-[4-(5-[(1E)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonybutanyol)amino]-1H-indol-2-yl]carbonyl]-Piperazine was synthesized by the two diferent synthetic routea from 5-nitroidole-2-carboxylic acid and resveratrol as the starting materials.The total yields were 15% and 24.5%,respectively.The structure of the key intermediates and target molecules was confirmed by MS, 1H NMR和13C NMR spectra in our experments.The route via amidation first,and then esterification was convenient and simple.