期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 17, 页码 5247-5253出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.06.046
关键词
CuAAC; Triazolobithiazole; Cystic fibrosis; CF corrector
资金
- National Institutes of Health [DK072517, GM089153, HL073856]
- National Science Foundation [CHE-0910870, CHE-0443516, CHE-0449845, CHE-9808183]
Copper catalyzed azide-alkyne cycloaddition (CuAAC) chemistry is reported for the construction of previously unknown 5-(1H-1,2,3-triazol-1-yl)-4,5'-bithiazoles from 2-bromo-1-(thiazol-5-yl)ethanones. These novel triazolobithiazoles are shown to have cystic fibrosis (CF) corrector activity and, compared to the benchmark bithiazole CF corrector corr-4a, improved log P values (4.5 vs 5.96). (C) 2012 Elsevier Ltd. All rights reserved.
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