CAJ | 학술논문

目的合成新型的非核苷类(双杂环苯基)化合物,并观察其抗HIV1-逆转录酶(HIV1-RT)活性.方法以氮芥盐酸盐为起始原料,与不同取代苯胺反应,得到相应的不同取代的哌嗪盐酸盐,并与1-溴-3-酞酰亚胺基-2-丁酮(4)缩合,得到目标化合物.结果合成11个目标化合物(5～15).经1HNMR,红外和元素分析确定结构.结论经HIV逆转录酶P-66蛋白测定,化合物11,14,10和13有一定抑制HIV1-RT活性,其IC50分别为29.80,35.20,43.77和63.76 μmol*L-1.
목적합성신형적비핵감류(쌍잡배분기)화합물,병관찰기항HIV1-역전록매(HIV1-RT)활성.방법이담개염산염위기시원료,여불동취대분알반응,득도상응적불동취대적고진염산염,병여1-추-3-태선아알기-2-정동(4)축합,득도목표화합물.결과합성11개목표화합물(5～15).경1HNMR,홍외화원소분석학정결구.결론경HIV역전록매P-66단백측정,화합물11,14,10화13유일정억제HIV1-RT활성,기IC50분별위29.80,35.20,43.77화63.76 μmol*L-1.
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 μmol*L-1, respectively.