title: Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines and their anti-HIV reverse transcriptase activity.
abstract: OBJECTIVE
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Chen
authors.forename: Lin
authors.initials: L
authors.lastname: Wang
authors.forename: Zhi-zhong
authors.initials: ZZ
authors.lastname: Zhao
authors.forename: Xing-quan
authors.initials: XQ
authors.lastname: Zhang
authors.forename: Xiang-hong
authors.initials: XH
authors.lastname: Chen
authors.forename: Hong-shan
authors.initials: HS
authors.lastname: Chen
mesh_terms: D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D010879:Piperazines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase