Abstract
Authorities of Drug Administration in the United States of America approved about 5000 drugs for use in the therapy or management of several diseases. About two hundred of these drugs have active metabolites and the knowledge of their medicinal chemistry is important both in medical practice and pharmaceutical research. This review gives a detailed description of the medicinal chemistry of drugs with active metabolites generated after conjugation. This review focused on glucuronide-, acetyl-, sulphate- and phosphate-conjugation of drugs, converting the drug into an active metabolite. This conversion essentially changed the lipophilicity of the drug.
Keywords: Prodrugs, metabolic conjugation, morphine-6-glucuronide, glucuronide conjugation, acetyl conjugation, sulphate conjugation, phosphate conjugation.
Mini-Reviews in Medicinal Chemistry
Title:Medicinal Chemistry of Drugs with Active Metabolites Following Conjugation
Volume: 13 Issue: 11
Author(s): Huba Kalász, Georg Petroianu, Sándor Hosztafi, Ferenc Darvas, Tamás Csermely, Ernest Adeghate, Afshan Siddiq and Kornélia Tekes
Affiliation:
Keywords: Prodrugs, metabolic conjugation, morphine-6-glucuronide, glucuronide conjugation, acetyl conjugation, sulphate conjugation, phosphate conjugation.
Abstract: Authorities of Drug Administration in the United States of America approved about 5000 drugs for use in the therapy or management of several diseases. About two hundred of these drugs have active metabolites and the knowledge of their medicinal chemistry is important both in medical practice and pharmaceutical research. This review gives a detailed description of the medicinal chemistry of drugs with active metabolites generated after conjugation. This review focused on glucuronide-, acetyl-, sulphate- and phosphate-conjugation of drugs, converting the drug into an active metabolite. This conversion essentially changed the lipophilicity of the drug.
Export Options
About this article
Cite this article as:
Kalász Huba, Petroianu Georg, Hosztafi Sándor, Darvas Ferenc, Csermely Tamás, Adeghate Ernest, Siddiq Afshan and Tekes Kornélia, Medicinal Chemistry of Drugs with Active Metabolites Following Conjugation, Mini-Reviews in Medicinal Chemistry 2013; 13 (11) . https://dx.doi.org/10.2174/1389557511313110002
DOI https://dx.doi.org/10.2174/1389557511313110002 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from 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
-
Characterization of Cancer Stem Cells and Primary Cilia in Medulloblastoma
CNS & Neurological Disorders - Drug Targets Epigenetic Regulation of Epithelial-Mesenchymal Transition by Hypoxia in Cancer: Targets and Therapy
Current Pharmaceutical Design Glutamate Transporter 1: Target for the Treatment of Alcohol Dependence
Current Medicinal Chemistry Expression, Distribution and Regulation of Phosphodiesterase 5
Current Pharmaceutical Design Exosomal microRNAs as Potentially Useful Tools in Cancer Biomarker Discovery
Recent Patents on Biomarkers Lipid-based siRNA Delivery Systems: Challenges, Promises and Solutions Along the Long Journey
Current Pharmaceutical Biotechnology Colloidal Supramolecular Aggregates for Therapeutic Application in Neuromedicine
Current Medicinal Chemistry Nanotools for the Delivery of Antimicrobial Peptides
Current Drug Targets Editorial (Thematic Issue: Emerging Concepts and Therapeutics Strategies for the Treatment of Brain Tumors)
Anti-Cancer Agents in Medicinal Chemistry TGF-ß / Smad Signaling in Prostate Cancer
Current Drug Targets miRNAs as Modulators of Cholesterol in Breast Cancer Stem Cells: An Approach to Overcome Drug Resistance in Cancer
Current Drug Targets Somatostatin, Somatostatin Analogs and Somatostatin Receptor Dynamics in the Biology of Cancer Progression
Current Molecular Medicine Recently Patented Applications of Homologous Cellular and Extracellular Agents as Therapeutics or Targets for the Prevention of Restenosis Post- Angioplasty
Recent Patents on Cardiovascular Drug Discovery α-Synuclein Misfolding and Neurodegenerative Diseases
Current Protein & Peptide Science Smad-Signaling in Mammary Gland Development and Tumorigenesis
Current Signal Transduction Therapy The Synthesis, Structural Modification and Mode of Anticancer Action of Evodiamine: A Review
Recent Patents on Anti-Cancer Drug Discovery A New Aspect of the TrkB Signaling Pathway in Neural Plasticity
Current Neuropharmacology Resveratrol Protects β Amyloid-Induced Oxidative Damage and Memory Associated Proteins in H19-7 Hippocampal Neuronal Cells
Current Alzheimer Research Editorial: Smart Drug Delivery Systems (Part 1)
Current Drug Targets Computational Insights into the Role of Glutathione in Oxidative Stress
Current Neurovascular Research