Synthesis and biological evaluation of 3-amino-2-pyrones as selective cyclooxygenase-1 (COX-1) inhibitors

A group of 3-amino-2-pyrones were synthesized and their biological activities were evaluated for inhibiting cyclooxygenase (COX) activity. This study has led to the identification of COX-1-selective inhibitors. Among the tested compounds, the compound 5j exhibited the most potent COX-1 inhibitory ac...

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Veröffentlicht in:Chinese chemical letters 2013-02, Vol.24 (2), p.120-122
Hauptverfasser: Chu, Xue-Ping, Zhou, Qing-Fa, Zhao, Shen, Ge, Fei-Fei, Fu, Mian, Chen, Jia-Peng, Lu, Tao
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Sprache:eng
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Zusammenfassung:A group of 3-amino-2-pyrones were synthesized and their biological activities were evaluated for inhibiting cyclooxygenase (COX) activity. This study has led to the identification of COX-1-selective inhibitors. Among the tested compounds, the compound 5j exhibited the most potent COX-1 inhibitory activity (IC50 =19.32mg/mL) and COX-1 selectivity index (SI;1;=41.98). A group of 3-amino-2-pyrones were synthesized and their biological activities were evaluated for inhibiting cyclooxygenase (COX) activity. This study has led to the identification of COX-1-selective inhibitors. Among the tested compounds, the compound 5j exhibited the most potent COX-1 inhibitory activity (IC50=19.32μg/mL) and COX-1 selectivity index (SI=41.98).
ISSN:1001-8417
1878-5964
DOI:10.1016/j.cclet.2013.01.005