Abstract
Peptidomimitism is applied to the medicinal chemistry in order to synthesize drugs that devoid of the disadvantages of peptides. AT1 antagonists constitute a new generation of drugs for the treatment of hypertension designed and synthesized to mimic the C-terminal segment of Angiotensin II and to block its binding action on AT1 receptor. An effort was made to understand the molecular basis of hypertension by studying the conformational analysis of Ang II and its derivatives as well as the AT1 antagonists belonging to SARTANs class of molecules. Such studies offer the possibility to reveal the stereoelectronic factors responsible for bioactivity of AT1 antagonists and to design and synthesize new analogs. An example will be given which proves that drugs with better pharmacological and financial profiles may arise based on this rational design.
Keywords: Antihypertensive Drugs, AT1 antagonists, C-terminal segment
Current Topics in Medicinal Chemistry
Title: Conformation and Bioactivity. Design and Discovery of Novel Antihypertensive Drugs
Volume: 4 Issue: 4
Author(s): T. Mavromoustakos, M. Zervou, P. Zoumpoulakis, I. Kyrikou, N. P. Benetis, L. Polevaya, P. Roumelioti, N. Giatas, A. Zoga and P. Moutevelis Minakakis
Affiliation:
Keywords: Antihypertensive Drugs, AT1 antagonists, C-terminal segment
Abstract: Peptidomimitism is applied to the medicinal chemistry in order to synthesize drugs that devoid of the disadvantages of peptides. AT1 antagonists constitute a new generation of drugs for the treatment of hypertension designed and synthesized to mimic the C-terminal segment of Angiotensin II and to block its binding action on AT1 receptor. An effort was made to understand the molecular basis of hypertension by studying the conformational analysis of Ang II and its derivatives as well as the AT1 antagonists belonging to SARTANs class of molecules. Such studies offer the possibility to reveal the stereoelectronic factors responsible for bioactivity of AT1 antagonists and to design and synthesize new analogs. An example will be given which proves that drugs with better pharmacological and financial profiles may arise based on this rational design.
Export Options
About this article
Cite this article as:
Mavromoustakos T., Zervou M., Zoumpoulakis P., Kyrikou I., Benetis P. N., Polevaya L., Roumelioti P., Giatas N., Zoga A. and Minakakis Moutevelis P., Conformation and Bioactivity. Design and Discovery of Novel Antihypertensive Drugs, Current Topics in Medicinal Chemistry 2004; 4 (4) . https://dx.doi.org/10.2174/1568026043451302
DOI https://dx.doi.org/10.2174/1568026043451302 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
- Announcements
Related Articles
-
Endothelial Dysfunction and Platelet Hyperaggregation in Type 2 Diabetes Mellitus: The Era of Novel Anti-diabetic Agents
Current Medicinal Chemistry Future Prospects in Anti-Platelet Therapy: A Review of Potential P2Y12 and Thrombin Receptor Antagonists
Recent Patents on Cardiovascular Drug Discovery Headache: One of the Most Common and Troublesome Adverse Reactions to Drugs
Current Drug Safety Management of the Menopausal Disturbances and Oxidative Stress
Current Pharmaceutical Design Alpinia calcarata Roscoe: A Rich Source of Phytopharmaceuticals in Sri Lanka
The Natural Products Journal The Potential Health Benefits of Algae and Micro Algae in Medicine: A Review on Spirulina platensis
Current Nutrition & Food Science Rheumatoid Arthritis: Cardiovascular Manifestations, Pathogenesis, and Therapy
Current Pharmaceutical Design The Potentials of Uncariae Ramulus Cum Uncis for the Treatment of Migraine: Targeting CGRP in the Trigeminovascular System
Current Neuropharmacology Objectively Assessed Physical Activity and Sedentary Behaviour During Pregnancy in Portuguese Women: Differences Between Trimesters and Weekdays and Weekends
Current Women`s Health Reviews Editorial (Thematic Issue: Polypharmacology in Drug Discovery)
Current Pharmaceutical Design Role of Nitrosative Stress and Peroxynitrite in the Pathogenesis of Diabetic Complications. Emerging New Therapeutical Strategies
Current Medicinal Chemistry The Effects of Glucose-Lowering Therapies on Diabetic Kidney Disease
Current Diabetes Reviews Novel Oral Anticoagulants in Peripheral Arterial and Coronary Artery Disease
Cardiovascular & Hematological Agents in Medicinal Chemistry Contribution of ALDH2 Polymorphism to Alcoholism-Associated Hypertension
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Associations between Adiponectin Gene Variability, Proinflammatory and Angiogenetic Markers: Implications for Microvascular Disease Development in Type 2 Diabetes Mellitus?
Current Vascular Pharmacology Editorial (Thematic Issue: ‘Lone’ Atrial Fibrillation: No Longer Lone or Even Alone)
Current Pharmaceutical Design Statins in Stroke Prevention: Present and Future
Current Pharmaceutical Design The Influence of Metabolism on the MAO-B Inhibitory Potency of Selegiline
Current Medicinal Chemistry Prevention and Treatment of Diabetic Retinopathy: Evidence from Large, Randomized Trials. The Emerging Role of Fenofibrate
Reviews on Recent Clinical Trials Renal Endothelial Dysfunction in Diabetic Nephropathy
Cardiovascular & Hematological Disorders-Drug Targets