SYNTHESIS OF 1-(3-PHTHALIMIDO-2-OXOBUTYL)-4-SUBSTITUTED-PHENYLPIPERAZINES AND THEIR ANTI-HIV REVERSE TRANSCRIPTASE ACTIVITY

AIMSynthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted-phenylpiperazines (5～15). METHODS The starting material nitrogen mustard hydrochloride (16), reacted with the corresponding substituted anilines to afford piperazine hydrochlorides (17～27), which were then coupled with 1-bromo-3-phthalimidobutan-2-one (4) to give the target compounds. RESULTS Eleven target compounds (5～15) were synthesized, which were characterized by 1HNMR, IR and elemental analysis. CONCLUSIONAnti-HIV-1 RT using HIV reverse transcriptase P-66 protein test showed that compounds 11, 14, 10 and 13 possessed inhibitory effects against HIV-1 reverse transcriptase (RT), with IC50 29.80, 35.20, 43.77 and 63.76 μmol·L^-1, respectively.