Synthesis, in vitro inhibitory activity towards COX-2 and haemolytic activity of derivatives of esculentoside A.

作者信息

Wu Fei, Yi Yanghua, Sun Peng, Zhang Dazhi

机构信息

Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.

出版信息

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6430-3. doi: 10.1016/j.bmcl.2007.10.006. Epub 2007 Oct 5.

DOI:10.1016/j.bmcl.2007.10.006

PMID:17950600

Abstract

Esculentoside A (EsA) has been reported to possess anti-inflammatory activity and selective inhibitory activity towards cyclooxygenase-2. A series of derivatives of EsA were synthesized by converting the C-28 carboxylic acid group into amides. The haemolytic activity and inhibitory activity towards cyclooxygenase-2 were evaluated in vitro. The SAR study of the derivatives was conducted and showed that introducing aromatic ring to EsA greatly enhanced its biological activity. Compound 23 showed higher inhibitory activity than Celecoxib and EsA, but lower haemolytic toxicity than EsA.

摘要

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