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
-
Losartan Chemistry and Its Effects via AT1 Mechanisms in the Kidney
Current Medicinal Chemistry Beta-propellers: Associated Functions and their Role in Human Diseases
Current Medicinal Chemistry Autoimmune Hepatitis
Current Pediatric Reviews Anti-Inflammatory Effects of Fibrates: An Overview
Current Medicinal Chemistry New Patents on Topical Anesthetics
Recent Patents on Inflammation & Allergy Drug Discovery Highly Resolution of Propranolol Using Oxidized Multi-walled Carbon Nanotubes and β-cyclodextrin Derivatives as Impregnating Reagents
Current Nanoscience Neuroprotective Effects of Ginkgolide B Against Ischemic Stroke: A Review of Current Literature
Current Topics in Medicinal Chemistry Axitinib in the Treatment of Head and Neck Malignancies
Current Clinical Pharmacology Sonic Hedgehog Signaling Activation Promotes Cardioprotective Strategies
Current Signal Transduction Therapy Effects of Highly Active Antiretroviral Therapy on Albuminuria in HIV-infected Persons
Infectious Disorders - Drug Targets Iptakalim Hydrochloride and Neuronal Protection
Current Neuropharmacology Patent Selections
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Recent Development on Anti-Obesity Compounds and their Mechanisms of Action: A Review
Current Medicinal Chemistry Cardiovascular Risk in Patients with Primary Hyperparathyroidism
Current Pharmaceutical Design Impact of Ivabradine on Health-Related Quality of Life of Patients with Ischaemic Chronic Heart Failure
Current Vascular Pharmacology Uric acid and Metabolic Syndrome: What is the Relationship?
Current Rheumatology Reviews An Overview of the Modulatory Effects of Oleic Acid in Health and Disease
Mini-Reviews in Medicinal Chemistry Vitamin D/VDR in Acute Kidney Injury: A Potential Therapeutic Target
Current Medicinal Chemistry Medical Treatment of Primary, Secondary, and Tertiary Hyperparathyroidism
Current Drug Safety An Overview on Application of Natural Substances Incorporated with Electrospun Nanofibrous Scaffolds to Development of Innovative Wound Dressings
Mini-Reviews in Medicinal Chemistry