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
-
Matrix Metalloproteinase Inhibitors as Prospective Agents for the Prevention and Treatment of Cardiovascular and Neoplastic Diseases
Current Topics in Medicinal Chemistry Dehydroepiandrosterone and Its Derivatives: Potentially Novel Anti-Proliferative and Chemopreventive Agents
Current Pharmaceutical Design Mechanochemical Approaches to Pharmaceutical Cocrystal Formation and Stability Analysis
Current Pharmaceutical Design Deciphering the Physiology Underlying the Rapid Clinical Effects of Perispinal Etanercept in Alzheimers Disease
Current Alzheimer Research Resistance to Anti-VEGF Agents
Current Pharmaceutical Design Therapeutic Interventions for Advanced Glycation-End Products and its Receptor- Mediated Cardiovascular Disease
Current Pharmaceutical Design Drug Metabolism and Transport Under Hypoxia
Current Drug Metabolism Adverse Drug Reactions in Hospitals: A Narrative Review
Current Drug Safety Drug-Targeting Strategies for Prostate Cancer
Current Pharmaceutical Design Phytochemicals Resveratrol and Sulforaphane as Potential Agents for Enhancing the Anti-Tumor Activities of Conventional Cancer Therapies
Current Pharmaceutical Biotechnology Current Insights into the Role of HIF-1 in Cutaneous Wound Healing
Current Molecular Medicine Electrotransfer into Skeletal Muscle for Protein Expression
Current Gene Therapy Uncontrolled Hypertension and Oncology: Clinical Tips
Current Vascular Pharmacology A Review of Statistical and Machine Learning Techniques for Microvascular Complications in Type 2 Diabetes
Current Diabetes Reviews Erythropoiesis Stimulating Agents and Anaemia of End-Stage Renal Disease
Cardiovascular & Hematological Agents in Medicinal Chemistry Embryonic Stem Cells: Overcoming the Immunological Barriers to Cell Replacement Therapy
Current Stem Cell Research & Therapy Oxidative Stress and Endothelial Dysfunction in Cardiovascular Disease: Mitochondria-Targeted Therapeutics
Current Medicinal Chemistry Biology of Transforming Growth Factor-β Signaling
Current Pharmaceutical Biotechnology Recommendations for Severe Hypertriglyceridemia Treatment, are there New Strategies?
Current Vascular Pharmacology QT Alterations in Psychopharmacology: Proven Candidates and Suspects
Current Drug Safety