Design, synthesis, and biological evaluation of pyrimidine-2-carboxamide analogs: investigation for novel RAGE inhibitors with reduced hydrophobicity and toxicity

被引：5
|
作者：
Kim, Seok-Ho [2 ]
Han, Young Taek [1 ]
机构：
[1] Dankook Univ, Coll Pharm, Cheonan 330714, South Korea
[2] CHA Univ, Coll Pharm, Pochen Si 487010, Gyeonggi Do, South Korea
来源：
ARCHIVES OF PHARMACAL RESEARCH | 2015年 / 38卷 / 11期
基金：
新加坡国家研究基金会;
关键词：
RAGE; RAGE inhibitor; Pyrimidine-2-carboxamide; Drug-like property; GLYCATION END-PRODUCTS; RECEPTOR; DISEASE;
D O I：
10.1007/s12272-015-0596-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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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页码：1952 / 1962
页数：11
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