Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines and their anti-HIV reverse transcriptase activity.
- Author:
Xin CHEN
1
;
Lin WANG
;
Zhi-zhong ZHAO
;
Xing-quan ZHANG
;
Xiang-hong CHEN
;
Hong-shan CHEN
Author Information
- Publication Type:Journal Article
- MeSH: HIV Reverse Transcriptase; antagonists & inhibitors; metabolism; Inhibitory Concentration 50; Molecular Structure; Piperazines; chemical synthesis; chemistry; pharmacology; Reverse Transcriptase Inhibitors; chemistry; pharmacology
- From: Acta Pharmaceutica Sinica 2002;37(5):343-347
- CountryChina
- Language:English
-
Abstract:
AIMSynthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines (5-15).
METHODSThe 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.
RESULTSEleven 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 mumol.L-1, respectively.
