Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines and their anti-HIV reverse transcriptase activity / 药学学报

ABSTRACT

<p><b>AIM</b>Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines (5-15).</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>Eleven target compounds (5-15) were synthesized, which were characterized by 1HNMR, IR and elemental analysis.</p><p><b>CONCLUSION</b>Anti-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 mumol.L-1, respectively.</p>