Abstract
By coupling nitric oxide (NO)-donating moieties with ATPT, an orally active AT1 receptor antagonist, a series of novel NO-releasing derivatives with N-phenylpyrrolyl-2-tetrazole moiety were designed and synthesized. The NOreleasing assay indicated that compound 4c had good maximum amount of NO release. Moreover the target compounds were evaluated for their antagonism of AT1 receptor with induced contraction in the rat thoracic aortic ring, and the results showed that compound 4c exhibited potent antagonistic activity of AT1 receptor, which was obviously superior to that of the control drug losartan. These results suggested that NO-donor ATPT hybrids may provide a promising approach for the search for novel antihypertensive agents.
Keywords: AT1 antagonist, anti-hypertension, ATPT, nitric oxide-donating.
Letters in Drug Design & Discovery
Title:Synthesis and Biological Evaluations of Novel Nitric Oxide-donating Derivatives of [1,2,4]triazol-5(4H)-one with N-phenylpyrrolyl-2-tetrazole Moiety as Anti-hypertension Candidates
Volume: 12 Issue: 3
Author(s): Yanchun Zhanga, Jichao Chen, Jinyi Xub*, Jinpei Zhou and Xiaoming Wu*
Affiliation:
- bDepartment of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China
- Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China
Keywords: AT1 antagonist, anti-hypertension, ATPT, nitric oxide-donating.
Abstract: By coupling nitric oxide (NO)-donating moieties with ATPT, an orally active AT1 receptor antagonist, a series of novel NO-releasing derivatives with N-phenylpyrrolyl-2-tetrazole moiety were designed and synthesized. The NOreleasing assay indicated that compound 4c had good maximum amount of NO release. Moreover the target compounds were evaluated for their antagonism of AT1 receptor with induced contraction in the rat thoracic aortic ring, and the results showed that compound 4c exhibited potent antagonistic activity of AT1 receptor, which was obviously superior to that of the control drug losartan. These results suggested that NO-donor ATPT hybrids may provide a promising approach for the search for novel antihypertensive agents.
Export Options
About this article
Cite this article as:
Zhanga Yanchun, Chen Jichao, Xub Jinyi*, Zhou Jinpei and Wu Xiaoming*, Synthesis and Biological Evaluations of Novel Nitric Oxide-donating Derivatives of [1,2,4]triazol-5(4H)-one with N-phenylpyrrolyl-2-tetrazole Moiety as Anti-hypertension Candidates, Letters in Drug Design & Discovery 2015; 12 (3) . https://dx.doi.org/10.2174/1570180811666141009235816
DOI https://dx.doi.org/10.2174/1570180811666141009235816 |
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
-
Renal Biopsy Research with Implications for Therapy of Glomerulonephritis
Current Drug Therapy Expanding Spectrum of Sodium Potassium Chloride Co-transporters in the Pathophysiology of Diseases
Current Neuropharmacology A Versatile Stability-indicating Liquid Chromatographic Method for the Simultaneous Determination of Atenolol, Hydrochlorothiazide and Chlorthalidone
Current Pharmaceutical Analysis Foreword [ Current Vascular Pharmacology is 10 Years Old! ]
Current Vascular Pharmacology The Role of Redox Dysregulation in the Inflammatory Response to Acute Myocardial Ischaemia-reperfusion Injury - Adding Fuel to the Fire
Current Medicinal Chemistry The Effect of Sex and Gender on Diabetic Complications
Current Diabetes Reviews Biology and Therapeutic Applications of Peroxisome Proliferator- Activated Receptors
Current Topics in Medicinal Chemistry Antiangiogenic Agents in the Treatment of HER2-Negative Metastatic breast Cancer: A Brief Review
Current Angiogenesis (Discontinued) Matrix Metalloproteinases and Colon Anastomosis Repair: A New Indication for Pharmacological Inhibition?
Mini-Reviews in Medicinal Chemistry COVID-19: An Update on Pathogenesis and Treatment
Current Pharmaceutical Design Identification of Inflammatory, Metabolic, and Cell Survival Pathways Contributing to Cerebral Small Vessel Disease by Postmortem Gene Expression Microarray
Current Neurovascular Research Results of Controlled Clinical Trials Comparing “Guideline Exposed” and “Guideline Naive” Physicians in the Treatment of Depression, Hypertension,and Diabetes: What can be Learned?
Current Psychiatry Reviews Antagonism by Bioactive Polyphenols Against Inflammation: A Systematic View
Inflammation & Allergy - Drug Targets (Discontinued) A Random Forest Model to Predict the Activity of a Large Set of Soluble Epoxide Hydrolase Inhibitors Solely Based on a Set of Simple Fragmental Descriptors
Combinatorial Chemistry & High Throughput Screening Implications of the Obesity Epidemic for Statin Therapy: Shifting Cholesterol Metabolism to a High Synthesis and Low Dietary Absorption State
Endocrine, Metabolic & Immune Disorders - Drug Targets Tyrosine Kinase Inhibitors – A Review on Pharmacology, Metabolism and Side Effects
Current Drug Metabolism Critical Roles of Insulin-Induced Senescence in Diabetic Vasculopathy
Vascular Disease Prevention (Discontinued) VIP in Neurological Diseases: More Than A Neuropeptide
Endocrine, Metabolic & Immune Disorders - Drug Targets Role of the Sympathetic Nervous Activity in Hypertension-Update in 2013
Current Hypertension Reviews A Clinician’s Guide to Monoamine Oxidase Inhibitors
Current Psychiatry Reviews