【摘要】 目前文献报道的非核苷类逆转录酶抑制剂(NNRTIs)共有50多类结构骨架,其中被FDA批准上市的药物只有nevirapine,delavirdine,efavirenz和etravirine 4种。由于HIV-1极易发生变异,第一代和第二代NNRTIs普遍产生耐药性,因此,抗耐药性成为新一代NNRTIs的必要条件。文中从活性较高、结构骨架多样的NNRTIs所具有的三维结构模型出发,概述了新一代NNRTIs发挥高效抗耐药性应具备的结构特点。Etravirine,rilpivirine,BILR 355 BS,GW695634,Capravirine以及部分三唑、四唑巯乙酰胺类化合物均具有这些特点,对野生型和突变型HIV-1都有很好的抑制作用。更多还原

【Abstract】 Currently,more than 50 different structures of non-nucleoside reverse transcriptase inhibitors(NNRTIs) have been found.Among them,nevirapine,delavirdine,efavirenz and etravirine are approved by FDA for the treatment of HIV-1 infection.For the mutations of HIV-1,rapid development of resistance to the drugs is the shortness of first and second generations of NNRTIs.Therefore,a new generation of NNRTIs must retain their potent activity against a wide range of drug resistant strains.In this review,we described the three-dimensional structural models of NNRTIs,and compared and analyzed the molecular structural features of the new generation of NNRTIs,including etravirine,rilpivirine,BILR 355 BS,GW695634,capravirine,triazole and tetrazole thioacetanilide analogues.更多还原