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Design,synthesis and activity evaluation of new anti-HIV-1 CXCR4 inhibitors

YE Jian-han;ZHOU Shang-min;WANG Qian;LU Lu;DONG Ming-xin;CHEN Hong-biao;JIANG Shi-bo;DAI Qiu-yun;College of Chemistry,Xiangtan University;Institute of Biotechnology,Academy of Military Medical Sciences;Key Laboratory of Medical Molecular Virology of Ministry of Education /Ministry of Public Health,Shanghai Medical College,Fudan University;  
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 CXCR4,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 by1 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).
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