期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 21, 页码 6172-6175出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.007
关键词
Complement inhibitors; Analogs of K76-COOH; Filifolinol; Bioactive small molecules; SAR
资金
- SECyT-UNR
- CONICET
- ANPCyT
A new series of tricyclic carboxylic acids with a 3H-spiro[benzofuran-2,10-cyclohexane] skeleton were synthesized from filifolinol, as analogs of the natural complement inhibitor K76-COOH. Their complement inhibitory activity was determined aiming to probe the importance of structural characteristics of the alicyclic part of K76-COOH. The presence and stereochemistry of O- and N-functionalities on C3' of the filifolinol derivatives are relevant for biological activity. The IC50 values of the most potent compounds were comparable or surpassed the activity of K76-COOH. The results also suggest that the diol moiety of the natural product may be useful for improving compound solubility. (c) 2009 Elsevier Ltd. All rights reserved.
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