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2-Hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 17:3208-3211
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
Abstract
- A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain.
- Subjects :
- Blood Glucose
ATP citrate lyase
Clinical Biochemistry
Pharmaceutical Science
ATP Citrate (pro-S)-Lyase
Biochemistry
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
Animals
Structure–activity relationship
Enzyme Inhibitors
Molecular Biology
Cells, Cultured
Triglycerides
chemistry.chemical_classification
Sulfonamides
biology
Triglyceride
Cholesterol
Body Weight
Organic Chemistry
Benzene
Lyase
Rats
Enzyme
Adipose Tissue
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Anti-Obesity Agents
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....863f1596275d02b6a6a0c62e58561a4d