Synthesis of an Anti-AIDs Drug Delavirdine Derivate, Resdelasu  

作　　者：GUAN Qing-xiang HE Li-peng WANG Xi ZHANG Wen-yan WANG En-si YU Xiang-hui 

机构地区：[1]School of Pharmacy, Jilin University, Changchun 130021, P. R. China [2]College of Life Science, Jilin University, Changchun 130012, P. R. China

出　　处：《Chemical Research in Chinese Universities》2008年第6期731-734,共4页高等学校化学研究（英文版）

基　　金：Supported by Scientific and Technological Development Program Foundation of Jilin Province, China(No.20020503-11)

摘　　要：In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[（1-methyl-ethyl）amino]-2-pyridinyl}-4-{ [5-（4-{5[（1E）-2-（hydroxyphenyl）ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino）-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by means of IH NMR, ~3C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield（46%） than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[（1-methyl-ethyl）amino]-2-pyridinyl}-4-{ [5-（4-{5[（1E）-2-（hydroxyphenyl）ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino）-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by means of IH NMR, ~3C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield（46%） than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.

关 键 词：Resdelasu Synthesis AIDs Conjugated compound 

分 类 号：TQ46[化学工程—制药化工]