Abstract
One of the enantiomers of a racemic drug may be pharmacologically inactive or toxic or ballast and, hence, U.S. FDA and European agencies have issued certain guidelines for marketing of optically active (homochiral) drugs. However, some homochiral drug enantiomers racemize in to human body leading to the generation of other antipodes, which may be toxic or ballast to the human beings. In addition, racemization reduces the administrated dosage concentration when the optically active enantiomer is converted into its inactive form. Therefore, racemization studies of homochiral drugs are the important and urgent need of today. This article reviews in vitro and in vivo racemization of homochiral drugs. The racemization of some homochiral drugs is described considering the affect of different variables such as temperature, concentration of the drug, ionic concentration, pH, addition of cyclodextrins, formation of inclusion complexes, etc. Efforts have also been made to discuss the mechanisms of the racemization process. Attempts have been made to suggest safe dosages of such drugs.
Keywords: Chiral drugs development, enantiomers, in vivo, in vitro, harmful affects, racemization
Combinatorial Chemistry & High Throughput Screening
Title: Homochiral Drug Design and Development by Racemization
Volume: 10 Issue: 5
Author(s): Imran Ali
Affiliation:
Keywords: Chiral drugs development, enantiomers, in vivo, in vitro, harmful affects, racemization
Abstract: One of the enantiomers of a racemic drug may be pharmacologically inactive or toxic or ballast and, hence, U.S. FDA and European agencies have issued certain guidelines for marketing of optically active (homochiral) drugs. However, some homochiral drug enantiomers racemize in to human body leading to the generation of other antipodes, which may be toxic or ballast to the human beings. In addition, racemization reduces the administrated dosage concentration when the optically active enantiomer is converted into its inactive form. Therefore, racemization studies of homochiral drugs are the important and urgent need of today. This article reviews in vitro and in vivo racemization of homochiral drugs. The racemization of some homochiral drugs is described considering the affect of different variables such as temperature, concentration of the drug, ionic concentration, pH, addition of cyclodextrins, formation of inclusion complexes, etc. Efforts have also been made to discuss the mechanisms of the racemization process. Attempts have been made to suggest safe dosages of such drugs.
Export Options
About this article
Cite this article as:
Ali Imran, Homochiral Drug Design and Development by Racemization, Combinatorial Chemistry & High Throughput Screening 2007; 10 (5) . https://dx.doi.org/10.2174/138620707781662835
DOI https://dx.doi.org/10.2174/138620707781662835 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...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
Related Articles
-
COX-2 Inhibition in Schizophrenia and Major Depression
Current Pharmaceutical Design Pharmacophore Based 3D-QSAR Modeling and Molecular Docking of Leucettines as Potent Dyrk1A Inhibitors
Letters in Drug Design & Discovery DJ-1: A New Comer in Parkinsons Disease Pathology
Current Molecular Medicine Editorial [Hot Topic: New Avenues of Research on Multiple Sclerosis from the Perspective of Chronic Cerebrospinal Venous Insufficiency Paradigm (Guest Editor: Marian Simka)]
Reviews on Recent Clinical Trials Targeting the JNK Signaling Pathway for Stroke and Parkinsons Diseases Therapy
Current Drug Targets - CNS & Neurological Disorders An Overview of HDAC Inhibitors and their Synthetic Routes
Current Topics in Medicinal Chemistry Etanercept Improves Cognitive Performance and Increases eNOS and BDNF Expression During Experimental Vascular Dementia in Streptozotocin- induced Diabetes
Current Neurovascular Research Neuropsychological Aspects of Dual Diagnosis
Current Drug Abuse Reviews Preface:
Current Pediatric Reviews Copper Binding Extrinsic to the Octarepeat Region in the Prion Protein
Current Protein & Peptide Science Perceptions in Type 1 Diabetes Mellitus with or Without the Use of Insulin Pump: An Online Study
Current Diabetes Reviews Road From Nose to Brain for Treatment of Alzheimer: The Bumps and Humps
CNS & Neurological Disorders - Drug Targets Vascular Endothelial Growth Factor (VEGF) Inhibition - A Critical Review
Anti-Cancer Agents in Medicinal Chemistry HIV-1 Subtypes B and C Tat Differentially Impact Synaptic Plasticity Expression and Implicates HIV-Associated Neurocognitive Disorders§
Current HIV Research Factors Promoting Tamoxifen Resistance in Breast Cancer via Stimulating Breast Cancer Stem Cell Expansion
Current Medicinal Chemistry Voxel-Based Morphometry of the Human Brain: Methods and Applications
Current Medical Imaging An EOG-based Vigilance Estimation Method Applied for Driver Fatigue Detection
Neuroscience and Biomedical Engineering (Discontinued) Effect of β-Blockers on Perioperative Myocardial Ischemia in Patients Undergoing Noncardiac Surgery
Current Drug Targets Editorial (Thematic Issue: Managing Strategies for Diverse Diseases: Challenges from Bench to Bedside Translation in Successful Drug Discovery and Development)
Current Pharmaceutical Design Strategies for Enhancing Progenitor Cell Mobilization and Function in Diabetes
Current Vascular Pharmacology