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-carbon...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.展开更多
基金Supported by Scientific and Technological Development Program Foundation of Jilin Province, China(No.20020503-11)
文摘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.
