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KMID : 0043320150380111952
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Archives of Pharmacal Research
2015 Volume.38 No. 11 p.1952 ~ p.1962
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Design, synthesis, and biological evaluation of pyrimidine-2-carboxamide analogs: investigation for novel RAGE inhibitors with reduced hydrophobicity and toxicity
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Kim Seok-Ho
Han Young-Taek
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Abstract
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This paper describes an investigation of novel RAGE inhibitors with improved drug-like properties. To identify the improved drug-like RAGE inhibitor, we designed and synthesized pyrimidine-2-carboxamide analogs based on our previous work. Several potent analogs with improved hydrophilicity were identified by evaluation of RAGE inhibitory activity. In particular, one of the potent (diethylamino)ethoxymethoxy analogs did not exhibit undesired cytotoxicity in contrast with the parent RAGE inhibitors.
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KEYWORD
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RAGE, RAGE inhibitor, Pyrimidine-2-carboxamide, Drug-like property
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