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Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and evaluation of potential prodrugs of lixazinone (N-cyclohexyl-N-methyl-4-[(1, 2, 3, 5-tetrahydro-2- …

…, R Alvarez, JJ Bruno, AM Strosberg, L Gu…

文献索引:Venuti, Michael C.; Alvarez, Robert; Bruno, John J.; Strosberg, Arthur M.; Gu, Leo; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 11 p. 2145 - 2152

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被引用次数: 14

摘要

The cyclic AMP phosphodiesterase (CAMP PDE) inhibitor and cardiotonic agent lixazinone (N-cyclohexyl-N-methyl-4-[(1, 2, 3, 5-tetrahydro-2-oxoimidazo [2, lb] quinazolin-7-yl) oxy] butyramide, RS-82856, 1) and its acid and base addition salts were found to be insufficiently soluble in formulations suitable for intravenous administration. These results prompted an investigation into potential prodrugs with enhanced aqueous solubility designed to deliver ...