Research And Synthesis Of A Key Intermediate Of HMOA With Anti-HIV Activity

AIDS is an acquired immune deficiency syndrome, which is caused by retrovirus HIV. Since the first cases of AIDS were identified in 1981, there are totally 70 million people infected with HIV, which killed 20 million. In 2002, an estimated 5 million people became newly infected with HIV among which 95 percent of the patients live in developing countries and 3.1 million died due to HIV. Although effective drugs are used in curing HIV, which had declined dead ratio, the number of people infected with HIV is increasing sharply in recent years. 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. NRTIs is a kind of drugs that had been developed for many years and there are many drugs belonging to NRTIs. It had been shown that NRTIs had strong inhibition activity with HIV. (+)-2R,5S-9-(2-Hydroxymethyl-1,3-oxathiolane-5-yl)-adenine(HMOA)is one of NRTIs and its antiviral and cytotoxicity assays were reported. Its median effective(EC50) and inhibitory(IC50) concentration in human peripheral blood mononuclear(PBM) cells and Vero Cells are 78.9μM, >100μM and >100μM respectively. And its EC50 of anti-HIV activity in MT-4 Cell line was 50μg·mL^-1 while its IC50 100μg·mL^-1. References showed that HMOA was synthesized from L-Gulose...