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2-(4-Carbonylphenyl)benzoxazole inhibitors of CETP: Scaffold design and advancement in HDLc-raising efficacy
- Source :
- Bioorganic & Medicinal Chemistry Letters. 21:1890-1895
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- The development of 2-phenylbenzoxazoles as inhibitors of cholesteryl ester transfer protein (CETP) is described. Initial efforts aimed at engineering replacements for the aniline substructures in the benchmark molecule. Reversing the connectivity of the central aniline lead to a new class of 2-(4-carbonylphenyl)benzoxazoles. Structure-activity studies at the C-7 and terminal pyridine ring allowed for the optimization of potency and HDLc-raising efficacy in this new class of inhibitors. These efforts lead to the discovery of benzoxazole 11v, which raised HDLc by 24 mg/dl in our transgenic mouse PD model.
- Subjects :
- Scaffold
Stereochemistry
medicine.drug_class
Clinical Biochemistry
Pharmaceutical Science
Mice, Transgenic
Carboxamide
Biochemistry
Chemical synthesis
Mice
Structure-Activity Relationship
chemistry.chemical_compound
In vivo
Drug Discovery
Cholesterylester transfer protein
medicine
Animals
Potency
Molecular Biology
Benzoxazoles
biology
Cholesterol, HDL
Organic Chemistry
Biological activity
Benzoxazole
Cholesterol Ester Transfer Proteins
chemistry
Drug Design
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....cd6a4e5b4fb86bec5c2667ebcf40fd52