【作者】 王力平； 邵倩芬； 何严萍； 陈芬儿；

【Author】 ~aWang Liping ~bShao Qianfen ~bHe Yanping ~bChen Fener Fudan Univ.~aCenter of Anal.& Measu.~bChem.Dept.Shanghai 200433

【机构】 复旦大学分析测试中心； 复旦大学化学系；

【摘要】 <正>获得性免疫缺陷综合征(Acquired immunodeficiency syndrom,AIDS)是由人类免疫缺陷病毒(Human immunodeficiency virues,HIV)引起流行性传染病,至今已有1600万人死于 AIDS。在 HIV 病毒的复制周期中,逆转录酶(RT)是 HIV 从 mRNA 转录 DNA 过程中起主导作用的酶, 因此 HIV-1 RT 成为开发抗 AIDS 药物的重要靶酶。HIV-1 RT 抑制剂从化学结构和作用机制上更多还原

【Abstract】 AIDS(Acquired immune deficiency syndrome)is caused by HIV(Human immunodeficiency virus).It attacks and destroys the body’s defense system that fights against infection,about 1600 0000 people were died of this disease.One of the key enzymes in the replication cycle of the HIV is the reverse transcriptase(RT),which is responsible for the conversion of mRNA viral genome to double DNA.Consequently,HIV-1 RT has emerged as prime target for the development of drugs for HIV/AIDS therapy.According to their chemical structure and interaction mechanism,inhibitors of HIV RT fall into two main classes:(1)Nucleoside inhibitors(NRTIs)and non-nucleoside inhibitors (NNRTIs).To date,more than thirty classes NNRTIs are reported,among them, 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine(HEPT),analogs attract peoples attention for their high biological activity,low toxicity and less drug resistance.Recently,we focus our effort on the modification of the N-land C-6positionofHEPT,and then design the compound 5-Isopropyl-6-(1-naphthylmethyl)-1-(-p-tolyl-carbonyl-methyl)uracil in attempt to finding more potent anti-HIV drugs.(Fig 1).更多还原