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.
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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 |
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