期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 6, 页码 1489-1494出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.09.002
关键词
C-Glycosides; Carbonic anhydrase; Phenol; Enzyme inhibition
资金
- EU grant (Metoxia)
- UNLP (Argentina)
- CONICET (Argentina)
A small series of C-cinnamoyl glycosides incorporating the phenol moiety has been prepared by reaction of glycosyl ketones with the appropriate benzaldehydes. Glycosides were tested for the inhibition of twelve mammalian isoforms of carbonic anhydrase. This is the first study in which alpha-CAs have been investigated for their interaction with C-glycosides, a novel carbohydrate scaffold in the design of carbonic anhydrase inhibitors. The C-cinnamoyl glycosides were generally effective CA inhibitors, with inhibition constants in the low micromolar range against CA I, II, IV, VA, VB, VI, VII, IX, XII, XIII, XIV and ineffective inhibitors of CA III. These results confirm that attaching carbohydrate moieties to CA phenol pharmacophore improves its inhibitory activity. (C) 2012 Elsevier Ltd. All rights reserved.
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