CAJ | 학술논문

目的：设计、合成一系列新型四氢喹啉-苄基或苯并咪唑多胺类化合物，作为潜在的靶向CXCR4辅助受体的新型抑制剂，并测定其抗HIV-1活性。方法组合HIV-1辅助受体CXCR4抑制剂三氮构效团与CCR5部分药效团，设计并合成一系列新化合物并经1 H-NMR、MS表征，用HIV-1ⅢB病毒测定化合物抑制活性。结果与结论设计合成的10个目标化合物未见文献报道。活性测试结果显示，四氢喹啉-苯并咪唑多胺类化合物具有较好的抗HIV活性（ IC50＜1μmol/L），四氢喹啉-苄基多胺类化合物活性较差（ IC50＞8μmol/L）。
목적：설계、합성일계렬신형사경규람-변기혹분병미서다알류화합물，작위잠재적파향CXCR4보조수체적신형억제제，병측정기항HIV-1활성。방법조합HIV-1보조수체CXCR4억제제삼담구효단여CCR5부분약효단，설계병합성일계렬신화합물병경1 H-NMR、MS표정，용HIV-1ⅢB병독측정화합물억제활성。결과여결론설계합성적10개목표화합물미견문헌보도。활성측시결과현시，사경규람-분병미서다알류화합물구유교호적항HIV활성（ IC50＜1μmol/L），사경규람-변기다알류화합물활성교차（ IC50＞8μmol/L）。
Objective To design and synthesize a series of new type four hydrogen quinoline-benzyl/benzimidazole amine derivatives as a potential new inhibitor targeting auxiliary receptor CXCR 4, and determine their inhibitory activities to HIV-1.Methods Based on HIV-1 receptor CXCR4 inhibitors containing three nitrogen structure-activity motif and CCR5 partial hydrophobic pharmacophore , a series of new compounds were designed , synthesized and characterized by 1 HNMR and MS.The inhibitory activities of these compounds were determined using HIV-1 IIIB virus.Results and Conclusion Ten target compounds are synthesized .Four hydrogen quinoline-benzimidazole amine derivatives exhibit good anti-HIV activity(IC50 <1 μmol/L), but four hydrogen quinoline-benzyl amine compounds are less active ((IC50 >8 μmol/L).