Abstract
We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzylpiperazin-1-yl)- N-(2-oxo-2,3-dihydrobenzooxazol-6-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit hearts. Several compounds were developed from and showed favorable activities compared with the standard drug milrinone. Compound 4l was the most potent with an increased stroke volume of 11.78 ± 0.18% (milrinone 6.36 ± 0.13%) at 1 10–4 M in our in-vitro study. The chronotropic effects of compounds having inotropic effects were also evaluated.
Keywords: 2, 3-Dihydro-2-oxobenzo[d]oxazole, Positive inotropic activity, Stroke volume
Medicinal Chemistry
Title:Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol- 6-yl)acetamides as Inotropic Agents
Volume: 8 Issue: 6
Author(s): Tianyi Zhang, Liangpeng Sun, Xuekun Liu, Xun Cui and Huri Piao
Affiliation:
Keywords: 2, 3-Dihydro-2-oxobenzo[d]oxazole, Positive inotropic activity, Stroke volume
Abstract: We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzylpiperazin-1-yl)- N-(2-oxo-2,3-dihydrobenzooxazol-6-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit hearts. Several compounds were developed from and showed favorable activities compared with the standard drug milrinone. Compound 4l was the most potent with an increased stroke volume of 11.78 ± 0.18% (milrinone 6.36 ± 0.13%) at 1 10–4 M in our in-vitro study. The chronotropic effects of compounds having inotropic effects were also evaluated.
Export Options
About this article
Cite this article as:
Zhang Tianyi, Sun Liangpeng, Liu Xuekun, Cui Xun and Piao Huri, Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol- 6-yl)acetamides as Inotropic Agents, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208061093
DOI https://dx.doi.org/10.2174/1573406411208061093 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
- 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
-
Effects of Erythropoietin on Brain Function
Current Pharmaceutical Biotechnology Angina in Women without Obstructive Coronary Artery Disease
Current Cardiology Reviews Interfering with Hedgehog Pathway: New Avenues for Targeted Therapy in Rhabdomyosarcoma
Current Drug Targets Diabetes, the Renin-Angiotensin System and Heart Disease
Current Vascular Pharmacology The Importance of Lost Minerals in Heart Failure
Cardiovascular & Hematological Agents in Medicinal Chemistry Developing New Anti-Arrhythmics: Clues from the Molecular Basis of Cardiac Ryanodine Receptor (RyR2) Ca2+-Release Channel Dysfunction
Current Pharmaceutical Design Management Of Elderly Patients With Diffuse Large B-Cell Lymphomas
Anti-Cancer Agents in Medicinal Chemistry An Efficient Attribute Reduction and Fuzzy Logic Classifier for Heart Disease and Diabetes Prediction
Recent Advances in Computer Science and Communications Use of Diverse Chemometric and Validation Methods to Accurately Predict Human Urotensin-II Receptor Antagonist Activity
Current Computer-Aided Drug Design Should Adipokines be Considered in the Choice of the Treatment of Obesity-Related Health Problems?
Current Drug Targets Perspective of Molecular Hydrogen in the Treatment of Sepsis
Current Pharmaceutical Design Development of Pin1 Inhibitors and their Potential as Therapeutic Agents
Current Medicinal Chemistry Protein Kinase C – Possible Therapeutic Target to Treat Cardiovascular Diseases
Cardiovascular & Hematological Disorders-Drug Targets Hyperglycemia and Perioperative Glucose Management
Current Pharmaceutical Design Nitroxyl (HNO): A Possible Strategy for Fighting Cancer
Current Topics in Medicinal Chemistry The Interaction Between Gender and Diabetes Mellitus in the Coronary Heart Disease Risk
Current Pharmaceutical Design Neuroprotective Methodologies of Co-Enzyme Q10 Mediated Brain Hemorrhagic Treatment: Clinical and Pre-Clinical Findings
CNS & Neurological Disorders - Drug Targets Mechanisms and Treatments of Oxidative Stress in Atrial Fibrillation
Current Pharmaceutical Design Perioperative Management of Patients on Adenosine Diphosphate Inhibitors in the Era of Drug-Eluting Stents: Review of the Literature and Clinical Implications
Current Medicinal Chemistry Nitric Oxide and Dietary Factors: Part IV Traditional Japanese Food (Soy Products, Fish and Tea)
Vascular Disease Prevention (Discontinued)