Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity

Analogues of 5,6-dihydroxypyrimidine (1a-1l, 2a-2c, 3a-3c) were synthesized and evaluated for their anti-HIV activity in vitro. Among all of the analogs, several compounds exhibited significant anti-HIV activity, especially 1b and 1e, which showed the most potent anti-HIV activity with EC50 values of 0.14 and 0.15 μM, and TI (therapeutic index) values of >300 and >900, respectively.