Abstract
In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2- azetidinone cholesterol absorption inhibitors have been synthesized, and all of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.
Keywords: 2-Azetidinone derivatives, Enantiomerically pure, Cholesterol absorption inhibition, Ezetimibe Analogs, Cholesterol, SAR, Ezetimibe(1), C-(3) sidechain, N-aryl ring, bio isosteric, β-lactam ring, CHD, serum
Letters in Drug Design & Discovery
Title: Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
Volume: 8 Issue: 6
Author(s): Yubin Wang, Haiqian, Wenlong Huang, Huibin Zhang and Jinpei Zhou
Affiliation:
Keywords: 2-Azetidinone derivatives, Enantiomerically pure, Cholesterol absorption inhibition, Ezetimibe Analogs, Cholesterol, SAR, Ezetimibe(1), C-(3) sidechain, N-aryl ring, bio isosteric, β-lactam ring, CHD, serum
Abstract: In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2- azetidinone cholesterol absorption inhibitors have been synthesized, and all of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.
Export Options
About this article
Cite this article as:
Wang Yubin, Haiqian , Huang Wenlong, Zhang Huibin and Zhou Jinpei, Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors, Letters in Drug Design & Discovery 2011; 8 (6) . https://dx.doi.org/10.2174/157018011795906776
DOI https://dx.doi.org/10.2174/157018011795906776 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
What does the Hospital Anxiety and Depression Scale (HADS) Really Measure in Liaison Psychiatry Settings?
Current Psychiatry Reviews Structural Chromosome Abnormalities Associated with Obesity: Report of Four New Subjects and Review of Literature
Current Genomics Atheroma Burden and Morphology in Women
Current Pharmaceutical Design Genetic Studies of Type 2 Diabetes in South Asians: A Systematic Overview
Current Diabetes Reviews Recent Insights into the Role of Prostanoids in Atherosclerotic Vascular Disease
Current Vascular Pharmacology Endothelial Dysfunction in Heart Failure: Mechanisms and Therapeutic Approaches
Current Vascular Pharmacology C-11 Radiochemistry in Cancer Imaging Applications
Current Topics in Medicinal Chemistry Evaluation of the Pulmonary Veins and Left Atrial Volume using Multidetector Computed Tomography in Patients Undergoing Catheter Ablation for Atrial Fibrillation
Current Cardiology Reviews Medicinal Agents in the Metabolic Syndrome
Cardiovascular & Hematological Agents in Medicinal Chemistry Why are People with “Poor Lung Function” At Increased Atherothrombotic Risk?A Critical Review with Potential Therapeutic Indications
Current Vascular Pharmacology Vitamin D and Metabolic Syndrome: Is There a Link?
Current Pharmaceutical Design Does Data Shape Moral Decision? Or Do Values Shape the Data?
Current Pediatric Reviews Dichotomous Life of DNA Binding High Mobility Group Box1 Protein in Human Health and Disease
Current Protein & Peptide Science The Pivotal Role of Nitric Oxide: Effects on the Nervous and Immune Systems
Current Pharmaceutical Design Improving of Nutraceutical Features of Many Important Mediterranean Vegetables by Inoculation with a New Commercial Product
Current Pharmaceutical Biotechnology Child Abuse and Neglect and its Psycho-Physical and Social Consequences: A Review of the Literature
Current Pediatric Reviews The Role of Drug Transporters in the Pharmacokinetics of Antibiotics
Current Drug Metabolism The Cardiovascular and Cardiac Actions of Ecstasy and its Metabolites
Current Pharmaceutical Biotechnology Ezetimibe and Vascular Endothelial Function
Current Vascular Pharmacology Biochemical and Histochemical Comparison of Cholinesterases in Normal and Alzheimer Brain Tissues
Current Alzheimer Research