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 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- 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
-
Impact of the Renin-Angiotensin-Aldosterone-System on Cardiovascular and Renal Complications in Diabetes Mellitus
Current Vascular Pharmacology Interaction of Nerve Agent Antidotes with Cholinergic Systems
Current Medicinal Chemistry An Update on Peptide Drugs for Voltage-Gated Calcium Channels
Recent Patents on CNS Drug Discovery (Discontinued) Effects of Hypertension, Diabetes Mellitus, Obesity and Other Factors on Kidney Haemodynamics
Current Vascular Pharmacology Moderate Hypothermia in the Management of Severe Traumatic Brain Injury: A Good Idea Proved Ineffective?
Current Pharmaceutical Design Designing Peptidomimetics
Current Topics in Medicinal Chemistry Preface [Hot Topic: Cytochrome P450 and Diseases: Implications in Drug Metabolism and Pathophysiology (Guest Editor: Vincent Pichette)]
Current Drug Metabolism Salt-Sensitive Hypertension: Perspectives on Intrarenal Mechanisms
Current Hypertension Reviews Malignant Hypercalcemia
Current Medicinal Chemistry The Role of Angiotensin-(1-7)/Mas Axis and Angiotensin Type 2 Receptors in the Central Nervous System in Cardiovascular Disease and Therapeutics: A Riddle to be Solved
Current Vascular Pharmacology Thromboxane A<sub>2</sub> Receptor Polymorphism in Association with Cerebral Infarction and its Regulation on Platelet Function
Current Neurovascular Research Towards Standardized Stem Cell Therapy in Type 2 Diabetes Mellitus: A Systematic Review
Current Stem Cell Research & Therapy The Potential of Flavonoids and Tannins from Medicinal Plants as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Editorial (Hot Topic: Marine Peptides: Emerging Perspectives for Pharmaceuticals)
Current Protein & Peptide Science The Beneficial Hemodynamic Actions of SGLT-2 Inhibitors beyond the Management of Hyperglycemia
Current Medicinal Chemistry Candesartan Cilexetil Microemulsions for Transdermal Delivery: Formulation, in-vitro Skin Permeation and Stability Assessment
Current Drug Delivery Chemotherapeutic Options for Colorectal Cancer Patients with Cardiovascular Diseases.
Reviews on Recent Clinical Trials The Role of Lifestyle Change in the Prevention and Treatment of NAFLD
Current Pharmaceutical Design Atherosclerosis and Arterial Blood Pressure in Mice
Current Drug Targets ACE2-Ang-(1-7)-Mas Axis in Brain: A Potential Target for Prevention and Treatment of Ischemic Stroke
Current Neuropharmacology