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Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines and their anti-HIV reverse transcriptase

Xin Chen¹, Lin Wang, Zhi-zhong Zhao

¹Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.

Yao Xue Xue Bao = Acta Pharmaceutica Sinica

|February 13, 2003

Abstract

Aim:

Synthesis 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.

Conclusion:

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.

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