SYNTHESIS AND COMPARATIVE ANTI-HIV ACTIVITIES OF NEW ACETYLATED 2',3'-DIDEOXY-3'-THIACYTIDINE ANALOGS

A series of prodrugs of 2',3'-dideoxy-3'-thiacytidine have been synthe sized in an effort to enhance the uptake of the prodrugs by HIV-1 infe cted cells and to increase the plasma half-life. The anti-HIV 1 activi ties of the new analogues and their cytotoxicities were determined in MT(4) cells. In vitro hydrolysis of the various drugs including retino ic acid derivatives, indicated that these agents were relatively stabl e toward plasma esterases. Most prodrugs with higher partition coeffic ients than 2',3'-dideoxy-3'-thiacytidine should diffuse into the cells to a greater extent.