期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 10, 页码 2364-2367出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.03.057
关键词
Maleic acid amide; pH-sensitivity; Degradability; Drug delivery
资金
- Seoul RBD program [ST110017M0209721]
- Mid-Career Researcher Program from Ministry of Science, ICT and Future Planning, Korea [NRF-2011-0013569]
- GAIA project - Ministry of Environment, Korea [G113-00055-3004-0]
We synthesized five maleic acid amide derivatives (maleic, citraconic, cis-aconitic, 2-(2'-carboxyethyl) maleic, 1-methyl-2-(2'-carboxyethyl) maleic acid amide), and compared their degradability for the future development of pH-sensitive biomaterials with tailored kinetics of the release of drugs, the change of charge density, and the degradation of scaffolds. The degradation kinetics was highly dependent upon the substituents on the cis-double bond. Among the maleic acid amide derivatives, 2-(2'-carboxyethyl) maleic acid amide with one carboxyethyl and one hydrogen substituent showed appropriate degradability at weakly acidic pH, and the additional carboxyl group can be used as a pH-sensitive linker. (C) 2014 Elsevier Ltd. All rights reserved.
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