ChemInform Abstract: Synthesis, Biological Evaluation, and Structure-Activity Relationships of 3-Acylindole-2-carboxylic Acids as Inhibitors of the Cytosolic Phospholipase A2.

✍ Scribed by M. LEHR

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 33 KB
• Volume: 28
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199749143

✦ Synopsis

1997 indole derivatives, isoindole derivatives indole derivatives, isoindole derivatives R 0140

49 -143

Synthesis, Biological Evaluation, and Structure-Activity Relationships of 3-Acylindole-2-carboxylic Acids as Inhibitors of the Cytosolic Phospholipase A2.

-All title compounds are synthesized by acylation and N-substitution of the corresponding indole-2-carboxylic acids in varying order, e.g. (IX) . Structure-activity relationship evaluations show that derivative (IX) has the highest potency of a series of derivatives of lead compound ( Ia), e.g. (I)-(IV) and (IX), due to its substituent at position 1 of the indole nucleus, and that it is about 20-fold more active than standard inhibitor arachidonyl trifluoromethyl ketone. -(LEHR, M.;