HIV inhibitors targeted at the reverse transcriptase.

摘要: HIV inhibitors targeted at the virus-associated reverse transcriptase (RT) can be divided into two groups, depending on whether they are substrate or nonsubstrate binding site. To first group belong 2′,3′-dideoxynucleosides (i.e., DDC, DDI), 3′-azido-2′,3′-dideoxynucleosides AZT), 3′-fluoro-2′,3′dideoxynucleosides FLT), 2′,3′-didehydro-2′,3′-dideoxynucleosides D4C, D4T) and carbocyclic derivatives thereof carbovir), 2′-fluoro-ara-2′,3′-dideoxynucleosides, 1,3-dioxolane 2′,3′-dideoxyl-3′-thiacytidine), oxetanocin analogues cyclobut-G) 9-(2-phosphonylmethoxyethyl)adenine (PMEA) 9-(3-fluoro-2-phosphonylmethoxypropyl)adenine (FPMPA) derivatives. These compounds need to phosphorylated intracellularly their triphosphate forms before act as competitive alternate substrates (chain terminators) of RT. The second includes tetrahydro-imidazo[4,5,l-jk][1,...