Design,synthesis and activity evaluation of new anti-HIV-1 CXCR4 inhibitors
10.7644/j.issn.1674-9960.2014.08.009
- VernacularTitle:CXCR4 HIV-1抑制剂的设计合成及活性研究
- Author:
Jianhan YE
;
Shangmin ZHOU
;
Qian WANG
;
Lu LU
;
Mingxin DONG
;
Hongbiao CHEN
;
Shibo JIANG
;
Qiuyun DAI
- Publication Type:Journal Article
- Keywords:
CXCR4;
HIV-1;
inhibitor;
synthesis;
activity
- From:
Military Medical Sciences
2014;(8):602-607
- CountryChina
- Language:Chinese
-
Abstract:
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).
