SCH-53823 AND SCH-53825, NOVEL FUNGAL METABOLITES WITH PHOSPHOLIPASE-D INHIBITORY ACTIVITY

Citation
M. Chu et al., SCH-53823 AND SCH-53825, NOVEL FUNGAL METABOLITES WITH PHOSPHOLIPASE-D INHIBITORY ACTIVITY, Bioorganic & medicinal chemistry letters, 6(5), 1996, pp. 579-584
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
6
Issue
5
Year of publication
1996
Pages
579 - 584
Database
ISI
SICI code
0960-894X(1996)6:5<579:SASNFM>2.0.ZU;2-J
Abstract
Two novel phospholipase D (PLD) inhibitors, Sch 53823 (1) and Sch 5382 5 (2), were isolated from a fungal culture. The acetylated derivatives , Sch 53827 (3) and Sch 53829 (4), were prepared for the purpose of st ructure determination. The extensive NMR studies of 3 and 4 including DEFT, COSY, NOESY, HETCOR, and selective INEPT experiments permitted t he establishment of their structures, as well as relative stereochemis tries. Among these compounds, 3 exhibited the most potent inhibitory a ctivity in the phospholipase D assay with the IC50 = 17 mu M.