Synthesis of Novel 5″-Substituted Tsao-T Analogues with Anti-Hiv-1 Activity

INTRODUCTION TSAO derivatives are potent and selective HIV-1 reverse transcriptase (HIV-1 RT) inhibitors. Although, structurally, they can be considered as highly functionalized nucleosides, they inhibit their target enzyme (HIV-1 RT) similarly to the so-called Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI).1-6 The different families of NNRTI, including TSAO, interact with the HIV-1 RT in a highly hydrophobic pocket, close but different from the active site, and several complexes of NNRTIs-HIV-1 RT have been resolved by X-ray crystallography.7-15