Design,Synthesis and Anti-HIV-1 Activity Evaluation of N-Benzamide Derivatives
ZHOU Meng1,2, LIAO Xiang-ming1,2, LIN Liang-cai1,2, ZHANG Rong-hong3, LI Rui4, XU Guo-bo1,2*
1. Engineering Research Center for the Development and Application of Ethnic Medicine and TCM [Ministry of Education] & National Engineering Research Center of Miao's Medicines, Guizhou Medcial University, Guiyang 550004, China; 2. School of Pharmacy, Guizhou Medical University, Guian 550025, China; 3. Tissue Engineering and Stem Cell Research Center, Guizhou Medical University, Guiyang 550004, China; 4. State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu 610041, China;
Abstract��OBJECTIVE To design and synthesize HIV-1 Vif inhibitor RN-18 derivatives and investigate their antiviral activities. METHODS RN-18 was used as the lead compound, and optimizations were carried out on the two side chains and the middle benzene ring. The anti-HIV-1 activities of the target compounds were analyzed by p24 assay, and the cytotoxicities of compounds with better activities were tested with MTT method. RESULTS Twenty-eight new derivatives were prepared, and their structures were characterized by MS and 1H-NMR. The activity test showed that the antiviral activities of seven compounds were obviously improved, and the activity of compound 26 was increased to be 11 times higher than that of RN-18, with an EC50 value of 21.8 ��mol��L-1. CONCLUSION Replacing the middle benzene ring of RN-18 with heterocycles generally improves the anti-HIV-1 activity, which provides the basis for further study.
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2018, Vol. 53 
