Design, Synthesis, and Biological Evaluation of Benzylamino-Methanone Based Cholesteryl Ester Transfer Protein Inhibitors

Autor: Areej Melhem, Ghassan Abu Sheikha, Ghadeer Albadawi, Reema Abu Khalaf
Jazyk: angličtina
Rok vydání: 2010
Předmět:
Models
Molecular
Quantitative structure–activity relationship
CETP inhibitors
high-density lipoprotein
pharmacophore modeling
quantitative structure-activity relationship
benzylamino-methanones
Stereochemistry
Pharmaceutical Science
Quantitative Structure-Activity Relationship
Article
Analytical Chemistry
lcsh:QD241-441
chemistry.chemical_compound
High-density lipoprotein
lcsh:Organic chemistry
Drug Discovery
Cholesterylester transfer protein
Benzyl Compounds
medicine
Animals
Physical and Theoretical Chemistry
chemistry.chemical_classification
biology
Organic Chemistry
medicine.disease
Benzoxazines
Cholesterol Ester Transfer Proteins
carbohydrates (lipids)
Biochemistry
chemistry
Design synthesis
Chemistry (miscellaneous)
biology.protein
Molecular Medicine
lipids (amino acids
peptides
and proteins)
Rabbits
Pharmacophore
Glycoprotein
Dyslipidemia
Lipoprotein
Zdroj: Molecules; Volume 15; Issue 8; Pages: 5721-5733
Molecules
Molecules, Vol 15, Iss 8, Pp 5721-5733 (2010)
ISSN: 1420-3049
DOI: 10.3390/molecules15085721
Popis: Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore its a proper target for treating dyslipidemia and related disorders. Guided by our previously-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 microM.
Databáze: OpenAIRE
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