1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2α: Bioisosteric replacement of the carboxylic acid and carboxamide moiety
| Autor: | Alwine Schulze Elfringhoff, Matthias Lehr, Mark Hess |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Blood Platelets
Spectrometry Mass Electrospray Ionization Indoles Magnetic Resonance Spectroscopy medicine.drug_class Stereochemistry Carboxylic acid Clinical Biochemistry Carboxylic Acids Pharmaceutical Science Carboxamide Phospholipase Biochemistry Chemical synthesis Phospholipases A Propane Structure-Activity Relationship chemistry.chemical_compound Cytosol Phospholipase A2 Drug Discovery medicine Humans Moiety Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Phospholipase A biology Group IV Phospholipases A2 Organic Chemistry Stereoisomerism chemistry biology.protein Molecular Medicine Indicators and Reagents Spectrophotometry Ultraviolet lipids (amino acids peptides and proteins) Bioisostere |
| Zdroj: | Bioorganic & Medicinal Chemistry. 15:2883-2891 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2007.02.016 |
| Popis: | Indole-5-carboxylic acids and -carboxamides with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent inhibitors of cytosolic phospholipase A(2)alpha (cPLA(2)alpha) isolated from human platelets. In continuation of our attempts to develop novel cPLA(2)alpha inhibitors, a number of derivatives of these substances characterized by bioisosteric replacement of the carboxylic acid and carboxamide functionality, respectively, were prepared. The results of the biological evaluation of the obtained compounds enabled us to gain further insight into structural features critical for cPLA(2)alpha inhibition. |
| Databáze: | OpenAIRE |
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