Abstract
Today, 75% of new drugs introduced to the market are single enantiomers and new techniques in asymmetric synthesis and chiral separation expedites chiral drug discovery and development worldwide. The enantiomers of a chiral drug present unique chemical and pharmacological behaviors in a chiral environment, such as the human body, in which the stereochemistry of chiral drugs determines their pharmacokinetic, pharmacodynamic, and toxicological actions. Thus, it is imperative that only the pure and therapeutically active isomer be prepared and marketed. Tuberculosis (TB), a highly contagious and airborne disease that is caused by infection with Mycobacterium tuberculosis (Mtb), currently represents one of the most threatening health problems globally. The emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB), as well as HIV co-infection along with a lengthy treatment regimen, highlights an urgent need for the development of new anti-TB agents. Currently, new chiral anti-TB agents are being developed from some well-known anti-TB agents, high throughput screening (HTS) hits, and natural products. This review will focus on the reported chiral anti-TB agents together with the clinical importance of their chirality and stereochemistry.
Keywords: Stereochemistry, chiral drugs, anti-tuberculosis agents, unique chemical and pharmacological behaviors, Tuberculosis (TB), contagious and airborne disease, Mycobacterium tuberculosis (Mtb), emergence of multidrug-resistant TB (MDR-TB), HIV co-infection, chiral anti-TB agents, high throughput screening (HTS), enantiopure biomolecules, racemic drug, enantiomers, dystomer
Current Topics in Medicinal Chemistry
Title: Stereochemistry at the Forefront in the Design and Discovery of Novel Anti-tuberculosis Agents
Volume: 11 Issue: 7
Author(s): Qingqing Huang, Rong He and Alan P. Kozikowski
Affiliation:
Keywords: Stereochemistry, chiral drugs, anti-tuberculosis agents, unique chemical and pharmacological behaviors, Tuberculosis (TB), contagious and airborne disease, Mycobacterium tuberculosis (Mtb), emergence of multidrug-resistant TB (MDR-TB), HIV co-infection, chiral anti-TB agents, high throughput screening (HTS), enantiopure biomolecules, racemic drug, enantiomers, dystomer
Abstract: Today, 75% of new drugs introduced to the market are single enantiomers and new techniques in asymmetric synthesis and chiral separation expedites chiral drug discovery and development worldwide. The enantiomers of a chiral drug present unique chemical and pharmacological behaviors in a chiral environment, such as the human body, in which the stereochemistry of chiral drugs determines their pharmacokinetic, pharmacodynamic, and toxicological actions. Thus, it is imperative that only the pure and therapeutically active isomer be prepared and marketed. Tuberculosis (TB), a highly contagious and airborne disease that is caused by infection with Mycobacterium tuberculosis (Mtb), currently represents one of the most threatening health problems globally. The emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB), as well as HIV co-infection along with a lengthy treatment regimen, highlights an urgent need for the development of new anti-TB agents. Currently, new chiral anti-TB agents are being developed from some well-known anti-TB agents, high throughput screening (HTS) hits, and natural products. This review will focus on the reported chiral anti-TB agents together with the clinical importance of their chirality and stereochemistry.
Export Options
About this article
Cite this article as:
Huang Qingqing, He Rong and P. Kozikowski Alan, Stereochemistry at the Forefront in the Design and Discovery of Novel Anti-tuberculosis Agents, Current Topics in Medicinal Chemistry 2011; 11 (7) . https://dx.doi.org/10.2174/156802611795165205
DOI https://dx.doi.org/10.2174/156802611795165205 |
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
-
Association of Folate Level in Blood with the Risk of Schizophrenia
Combinatorial Chemistry & High Throughput Screening Biological Properties of Yeast-based Mannoprotein for Prospective Biomedical Applications
Combinatorial Chemistry & High Throughput Screening The Role of Ketamine in Treatment-Resistant Depression: A Systematic Review
Current Neuropharmacology Pulmonary Vaccine Delivery Systems: A Novel Approach for Immunization
Current Drug Therapy Antiviral Activity and Molecular Targets of Plant Natural Products Against Avian Influenza Virus
Current Organic Chemistry Human Tuberculosis I. Epidemiology, Diagnosis and Pathogenetic Mechanisms
Current Medicinal Chemistry Chemical Constituents and Biological Significance of the Genus Ilex (Aquifoliaceae)
The Natural Products Journal Therapeutic Vaccines Explored in Patients with Non-Small Cell Lung Cancer
Anti-Cancer Agents in Medicinal Chemistry The α/β Hydrolase Fold Proteins of Mycobacterium tuberculosis, with Reference to their Contribution to Virulence
Current Protein & Peptide Science Systemic Treatments for Adult Patients with Moderate-to-Severe Psoriasis: Consensus Statements for the United Arab Emirates
New Emirates Medical Journal Phage Choice, Isolation, and Preparation for Phage Therapy
Current Pharmaceutical Biotechnology Tofacitinib, an Oral Janus Kinase Inhibitor: Perspectives in Dermatology
Current Medicinal Chemistry A Review: The Anti-inflammatory, Anticancer and Antibacterial Properties of Four Kinds of Licorice Flavonoids Isolated from Licorice
Current Medicinal Chemistry Structural Characterization, Biological Effects, and Synthetic Studies on Xanthones from Mangosteen (Garcinia mangostana), a Popular Botanical Dietary Supplement
Mini-Reviews in Organic Chemistry In Vitro Drug Release Behavior, Mechanism and Antimicrobial Activity of Rifampicin Loaded Low Molecular Weight PLGA-PEG-PLGA Triblock Copolymeric Nanospheres
Current Drug Delivery High Levels of CD57+CD28- T-Cells, Low T-Cell Proliferation and Preferential Expansion of Terminally Differentiated CD4+ T-Cells in HIVElite Controllers
Current HIV Research Tumor Necrosis Factor: How to Make a Killer Molecule Tumor-Specific?
Current Cancer Drug Targets Synthetic Thioamide, Benzimidazole, Quinolone and Derivatives with Carboxylic Acid and Ester Moieties: A Strategy in the Design of Antituberculosis Agents
Current Medicinal Chemistry Anti-Inflammatory Therapy in Uveitis
Recent Patents on Inflammation & Allergy Drug Discovery Nanocarriers as Prospective Approach in Effective Management of Acne Vulgaris
Micro and Nanosystems