Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl esters as prodrugs of carboxylic acid agents

E Mendes, T Furtado, J Neres, J Iley, T Jarvinen…

文献索引：Mendes, Eduarda; Furtado, Tania; Neres, Joao; Iley, Jim; Jarvinen, Tomi; Rautio, Jarkko; Moreira, Rui Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 3 p. 809 - 816

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被引用次数: 17

摘要

Aminocarbonyloxymethyl esters 3 based on (S)-amino acid carriers were synthesised and evaluated as potential prodrugs of carboxylic acid agents. In addition, the compounds were evaluated as topical prodrugs with the aim of improving the dermal delivery of two non- steroidal anti-inflammatory agents: naproxen and flufenamic acid. The lipophilicities of these compounds were determined and their hydrolyses in aqueous solutions and in human ...