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
-
Salvia species, Interesting Plants Offering Perspectives in Alzheimer’s Disease
Current Traditional Medicine Nucleic Acids as Therapeutic Agents
Current Topics in Medicinal Chemistry Reliability and Validity of the Comprehensive Assessment of the at Risk Mental State, Italian Version (CAARMS-I)
Current Pharmaceutical Design CREG: A Possible Candidate for Both Prevention and Treatment of Proliferative Vascular Disease
Current Molecular Medicine Beyond the Synapse and Hebb's Rule: Is the Rest of the Neuron More Important for Psychiatric Disorders?
Current Psychiatry Reviews Hybrid High Exploration Particle Swarm Optimization Algorithm Improves the Prediction of the 2-Dimensional Hydrophobic-Polar Model for Protein Folding
Current Bioinformatics Patent Selections:
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Molecular Iodine in the Synthesis of Chromone-type Compounds
Current Organic Synthesis Approaches to Target Profiling of Natural Products
Current Medicinal Chemistry Lipid-Based Nanocarriers for CNS-Targeted Drug Delivery
Recent Patents on CNS Drug Discovery (Discontinued) Perioperative Considerations in Diabetic Patients
Current Diabetes Reviews Exosomes: A Novel Therapeutic Paradigm for the Treatment of Depression
Current Drug Targets Dopamine: The Forgotten Felon in Type 2 Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Anhedonia and Increased Stress Sensitivity: Two Promising Endophenotypes for Major Depression
Current Psychiatry Reviews Nanoceuticals as an Emerging Field: Current Status and Future Prospective
Current Nutrition & Food Science The Role of B Cells in Multiple Sclerosis: Implications for B-Cell-Targeted Therapy
Current Medicinal Chemistry Enzyme Inhibitors as the Attractive Targets for the Treatment of Various Diseases
Current Medicinal Chemistry Radiotracers for Amyloid Imaging in Neurodegenerative Disease: State-of-the-Art and Novel Concepts
Current Medicinal Chemistry miR-126 as a Therapeutic Agent for Diabetes Mellitus
Current Pharmaceutical Design Endocannabinoids in Neuroimmunology and Stress
Current Drug Targets - CNS & Neurological Disorders