Synthesis of an Anti-AIDs Drug Delavirdine Derivate, Resdelasu

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-carbonylbu- tanoyl}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 1H NMR, 13C 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.