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
-
Nasal Vaccines Against Hepatitis B: An Update
Current Pharmaceutical Biotechnology Development and Validation of a Liquid Chromatographic Method for Aroylhydrazones at Hydrolytic Conditions
Current Pharmaceutical Analysis Tumor Markers in Patients with Benign and Malignant Pulmonary Diseases; Competitive Evaluation of ProGRP, NSE and Cyfra 21-1
Recent Patents on Biomarkers IL-6 Signaling and its Blockade with a Humanized Anti-Interleukin-6 Receptor Antibody in Rheumatoid Arthritis: Advent of a New and Innovative Therapeutic Drug, Tocilizumab
Current Rheumatology Reviews Anti-VEGF Therapy for Retinal Vein Occlusions
Current Drug Targets Molecular Docking, Metal Substitution and Hydrolysis Reaction of Chiral Substrates of Phosphotriesterase
Combinatorial Chemistry & High Throughput Screening Toward the Virtual Screening of Potential Drugs in the Homology Modeled NAD+ Dependent DNA Ligase from Mycobacterium tuberculosis
Protein & Peptide Letters Antimicrobial and Biofilm Inhibiting Diketopiperazines
Current Medicinal Chemistry The Impact of Infection on the Incidence of Autoimmune Disease
Current Topics in Medicinal Chemistry Small Molecules Modulating Biogenesis or Processing of microRNAs with Therapeutic Potentials
Current Medicinal Chemistry Recent Applications of Doebner, Doebner-von Miller and Knoevenagel-Doebner Reactions in Organic Syntheses
Current Organic Synthesis Substituted Naphthalen-1-yl-Acetic Acid Hydrazides: Synthesis, Antimicrobial Evaluation and QSAR Analysis
Medicinal Chemistry Drugs Targeting Parasite Lysosomes
Current Pharmaceutical Design Recent Achievements on Siderophore Production and Application
Recent Patents on Biotechnology Editorial
Infectious Disorders - Drug Targets Diagnosis and Treatment of Pulmonary Fungal Infections in Critically Ill Patients
Current Respiratory Medicine Reviews Identifying Key Regulator Genes for Tuberculosis by Differential Co- Expression Analysis of Gene Expression Profiling
Current Bioinformatics A Comprehensive Systemic Literature Review of Pericardial Decompression Syndrome: Often Unrecognized and Potentially Fatal Syndrome
Current Cardiology Reviews Antibiotic Sensitivity of Bacillus clausii Strains in Commercial Preparation
Clinical Immunology, Endocrine & Metabolic Drugs (Discontinued) Biological and Chemical Diversity of Coral-Derived Microorganisms
Current Medicinal Chemistry