The Benefits and Challenges of Chlorine Substitution in Enhancing Drug Efficacy and Stability

In recent years, chlorine substitution has become an important method in drug improvement and design. This method allows for enhanced efficacy and metabolic stability in various pharmaceutical compounds. Studies on chlorine substitution, such ketamine and fluoroquinolones, highlight the role of halogens in improving drug-target interactions and increasing the longevity of drugs in the body. Despite the advantages it brings, concerns related to drug clearance and the risk of bioaccumulation remain ongoing areas of research. This article briefly introduces how chlorine affects the hydrophobicity of drugs, enhances metabolic stability, and increases binding affinity, resulting in improved drug efficacy. It also uses examples like ketamine and fluoroquinolones to show these effects. However, it also highlights limitations, such as slower drug clearance and potential toxicity. The article provides an understanding of key mechanisms, including the benefits and risks, to help those interested in biochemistry understand its impact at the molecular level. Future studies could focus on balancing metabolic stability with clearance efficiency and expanding research to explore how other halogens, such as fluorine and bromine, can help in drug modification, including their effects on binding affinity, metabolic stability, and toxicity.

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Publication Details

Journal
Theoretical and Natural Science
Published
2025-01-15
DOI
https://doi.org/10.54254/2753-8818/2025.20140
Primary Topic
Pharmacogenetics and Drug Metabolism
Type
article
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article

The Benefits and Challenges of Chlorine Substitution in Enhancing Drug Efficacy and Stability

Zhilei Shan
Theoretical and Natural Science
Pharmacogenetics and Drug Metabolism
article

The Benefits and Challenges of Chlorine Substitution in Enhancing Drug Efficacy and Stability

Zhilei Shan
article en

Abstract

In recent years, chlorine substitution has become an important method in drug improvement and design. This method allows for enhanced efficacy and metabolic stability in various pharmaceutical compounds. Studies on chlorine substitution, such ketamine and fluoroquinolones, highlight the role of halogens in improving drug-target interactions and increasing the longevity of drugs in the body. Despite the advantages it brings, concerns related to drug clearance and the risk of bioaccumulation remain ongoing areas of research. This article briefly introduces how chlorine affects the hydrophobicity of drugs, enhances metabolic stability, and increases binding affinity, resulting in improved drug efficacy. It also uses examples like ketamine and fluoroquinolones to show these effects. However, it also highlights limitations, such as slower drug clearance and potential toxicity. The article provides an understanding of key mechanisms, including the benefits and risks, to help those interested in biochemistry understand its impact at the molecular level. Future studies could focus on balancing metabolic stability with clearance efficiency and expanding research to explore how other halogens, such as fluorine and bromine, can help in drug modification, including their effects on binding affinity, metabolic stability, and toxicity.

Theoretical and Natural ScienceVol. 85(1)
Santa Clara University (US)
Good health and well-being
Openalex Percentile: Top 73%
Pharmacogenetics and Drug Metabolism
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The Benefits and Challenges of Chlorine Substitution in Enhancing Drug Efficacy and Stability — Zhilei Shan · Theoretical and Natural Science (2025) | TGRS Research Map | TGRS