Novel inhibitors of fatty acid oxidation as potential metabolic modulators
| Autor: | Tim Marquart, Dewan Zeng, Elfatih Elzein, Suresh S. Kerwar, Nancy Chu, Daniel Soohoo, Prabha Ibrahim, Kevin D. Shenk, Stephanie Meyer, Jeff Zablocki, Kwan Leung, Shirley Wong, Hiba Ahmed |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Stereochemistry
medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide Mitochondrion Biochemistry Chemical synthesis Mitochondria Heart chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Animals Humans Molecular Biology IC50 Beta oxidation Alkyl chemistry.chemical_classification Molecular Structure Palmitoyl Coenzyme A Chemistry Organic Chemistry Fatty Acids Biological activity Rats Piperazine Liver Microsomes Liver Molecular Medicine Epoxy Compounds Oxidation-Reduction |
| Zdroj: | Bioorganicmedicinal chemistry letters. 14(4) |
| ISSN: | 0960-894X |
| Popis: | We describe the synthesis of novel inhibitors of fatty acid oxidation as potential metabolic modulators for the treatment of stable angina. Replacement of the 2H-benzo[d]1,3-dioxolene ring system in our initial lead 3 with different benzthiazoles, benzoxazoles and introducing small alkyl substituents into the piperazine ring resulted in analogues with enhanced inhibitory activity against 1-14[C]-palmitoyl-CoA oxidation in isolated rat heart mitochondria (6, IC50=70 nM; 25, IC50=23 nM). |
| Databáze: | OpenAIRE |
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