Abstract
Sixteen 2-azetidinones were designed and synthesized as cholesterol absorption inhibitors. The length of C-3 side chain was modified to four atoms by introducing ester or amide linkage to investigate further structure-activity relationships. The target compounds exhibited different cholesterol absorption inhibition activities, some of which were promising.
Keywords: 2-Azetidinone, Cholesterol absorption inhibitor, NPC1L1, Ezetimibe, Bioactivities, Structure-activity relationship
Letters in Drug Design & Discovery
Title: Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors
Volume: 6 Issue: 6
Author(s): Jianfeng Ji, Rui Zhao, Wenlong Huang, Huibin Zhang, Jinpei Zhou, Yubin Wang and Hai Qian
Affiliation:
Keywords: 2-Azetidinone, Cholesterol absorption inhibitor, NPC1L1, Ezetimibe, Bioactivities, Structure-activity relationship
Abstract: Sixteen 2-azetidinones were designed and synthesized as cholesterol absorption inhibitors. The length of C-3 side chain was modified to four atoms by introducing ester or amide linkage to investigate further structure-activity relationships. The target compounds exhibited different cholesterol absorption inhibition activities, some of which were promising.
Export Options
About this article
Cite this article as:
Ji Jianfeng, Zhao Rui, Huang Wenlong, Zhang Huibin, Zhou Jinpei, Wang Yubin and Qian Hai, Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors, Letters in Drug Design & Discovery 2009; 6 (6) . https://dx.doi.org/10.2174/157018009789057562
DOI https://dx.doi.org/10.2174/157018009789057562 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
Related Journals
Related Books
- 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
-
Carotid Ultrasound in One, Two and Three Dimensions
Vascular Disease Prevention (Discontinued) Disease Modifying Osteoarthritis Drugs: Facing Development Challenges and Choosing Molecular Targets
Current Drug Targets Nanotechnological Strategies for the Treatment of Neglected Diseases
Current Pharmaceutical Design A Genome-wide Association Analysis in Four Populations Reveals Strong Genetic Heterogeneity For Birth Weight
Current Genomics The Role of the Metabolism of Anticancer Drugs in Their Induced-Cardiotoxicity
Current Drug Metabolism Mean Platelet Volume: A Link Between Thrombosis and Inflammation?
Current Pharmaceutical Design A Study of Metabolic Parameters in Patients with Gout: A Single Center Study from Nepal
Endocrine, Metabolic & Immune Disorders - Drug Targets Adonis sp., Convallaria sp., Strophanthus sp., Thevetia sp., and Leonurus sp. - Cardiotonic Plants with Known Traditional Use and a Few Preclinical and Clinical Studies
Current Pharmaceutical Design Current Research on Opioid Receptor Function
Current Drug Targets Development and Characterization of Spray Dried Microparticles for Pulmonary Delivery of Antifungal Drug
Current Drug Delivery Green Tea Attenuates Cardiovascular Remodeling and Metabolic Symptoms in High Carbohydrate-Fed Rats
Current Pharmaceutical Biotechnology Meet Our Associate Editor
Current Cardiology Reviews ApoE4 May be a Promising Target for Treatment of Coronary Heart Disease and Alzheimer's Disease
Current Drug Targets Diminished Renal Function and the Incidence of Heart Failure
Current Cardiology Reviews Consumption of Polyphenol Plants May Slow Aging and Associated Diseases
Current Pharmaceutical Design Editorial (Thematic Issue: Modifying Cardiovascular Risk Factors: Newer Advances in Cardiovascular Metabolism and Diagnostic Technologies)
Current Pharmaceutical Design Prophylactic Vaccine Approach for Colon and Pancreatic Cancers: Present and Future
Current Medicinal Chemistry Non-Vitamin K Oral Anticoagulants (NOACs) A Review of Clinical Management and Laboratory Issues
Current Vascular Pharmacology Nutlin-3, A p53-Mdm2 Antagonist for Nasopharyngeal Carcinoma Treatment
Mini-Reviews in Medicinal Chemistry Clinical Implications of Non-Invasive Measurement of Central Aortic Blood Pressure
Current Vascular Pharmacology