Phenolic diterpenoid derivatives as anti-influenza a virus agents
A series of diterpenoid derivatives based on podocarpic acid were synthesized and evaluated as anti-influenza A virus agents. Several of the novel podocarpic acid derivatives exhibited nanomolar activities against an H1N1 influenza A virus (A/Puerto Rico/8/34) that was resistant to two anti-influenza drugs, oseltamivir and amantadine. This class of compounds inhibits the influenza virus by targeting the viral hemagglutinin-mediated membrane fusion. These results indicated that podocarpic acid derivatives may serve as potential drug candidates to fight drug-resistant influenza A virus infections.
Dang, Zhao,Jung, Katherine,Zhu, Lei,Xie, Hua,Lee, Kuo-Hsiung,Chen, Chin-Ho,Huang, Li
supporting information
p. 355 - 358
(2015/03/30)
A general procedure for the esterification of carboxylic acids with diazoalkanes generated in situ by the oxidation of N-tert- butyldimethylsilylhydrazones with (difluoroiodo)benzene
The bimolecular reaction of carboxylic acids with diazoalkanes to form esters is among the mildest and most efficient of organic transformations but is seldom used in synthesis beyond the important case of methyl esterification. This is largely a consequence of the inaccessibility and poor stability of higher diazoalkanes as substrates. In this work we describe a new method for the synthesis of diazoalkanes by the oxidation of N-tert-butyldimethylsilylhydrazones (TBSHs) with (difluoroiodo)benzene, a reagent heretofore unexplored in the context of hydrazone oxidation. When conducted in the presence of a carboxylic acid substrate, the oxidation leads to efficient esterification in situ. In addition to greatly extending the range of diazoalkanes that are now available for esterifications, this new protocol offers significant advantages with regard to safety, for diazo intermediates are neither isolated nor achieve appreciable concentrations during the reaction. Copyright
Furrow, Michael E.,Myers, Andrew G.
p. 12222 - 12223
(2007/10/03)
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