Click chemistry in drug development recent trends and application

K. Barry Sharpless invented click chemistry in 2001, and it has revolutionized drug development with its effective, diverse, and selective chemical synthesis. In fact, the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) process has become a crucial tool for drug-like particle assembly, functionalization of physiologically active mixtures, and accurate drug-biomolecule conjugation. Late-stage click chemistry applications span a number of industries, including prodrugs, antibody-drug conjugates (ADCs), and specific drug delivery systems including hydrogels and nanoparticles. Click reactions' high specificity and bio-orthogonality have increased therapeutic precision, lessening side effects and improving therapeutic outcomes. New reactions, such as sulfur-fluoride exchange (SuFEx) and strain-promoted azide-alkyne cycloaddition (SPAAC), are a part of emerging trends in click chemistry that expand the range of applications. Click chemistry has improved lead compound synthesis, made it easier to develop pharmacophore linkers, and produced bio isosteres to improve drug potency and metabolic stability in the drug discovery process. The method's role in creating cutting-edge treatments has also been highlighted by its contribution to the discovery of inhibitors for diseases like HIV, cancerous development, and bacterial infections. From early stage drug discovery to clinical development, click chemistry remains at the forefront of pharmaceutical analysis, highlighting its critical influence on ongoing drug development.

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Publication Details

Journal
Research Journal of Pharmacy and Technology
Published
2025-05-07
DOI
https://doi.org/10.52711/0974-360x.2025.00345
Primary Topic
Click Chemistry and Applications
Type
article
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article

Click chemistry in drug development recent trends and application

Kamini Vijeepallam, Murali Sundaram, Thanapakiam Ganeson, U.S. Mahadeva Rao et al.
Research Journal of Pharmacy and Technology
Click Chemistry and Applications
article

Click chemistry in drug development recent trends and application

Kamini Vijeepallam, Murali Sundaram, Thanapakiam Ganeson, U.S. Mahadeva Rao, K. A. Ameer, Nikhil Nikhil, Vinoth Kumar Selvaraj, Anchal Guleria, Lee Wan Zhen, Venketash Kumar Krishnamoorthy
article en

Abstract

K. Barry Sharpless invented click chemistry in 2001, and it has revolutionized drug development with its effective, diverse, and selective chemical synthesis. In fact, the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) process has become a crucial tool for drug-like particle assembly, functionalization of physiologically active mixtures, and accurate drug-biomolecule conjugation. Late-stage click chemistry applications span a number of industries, including prodrugs, antibody-drug conjugates (ADCs), and specific drug delivery systems including hydrogels and nanoparticles. Click reactions' high specificity and bio-orthogonality have increased therapeutic precision, lessening side effects and improving therapeutic outcomes. New reactions, such as sulfur-fluoride exchange (SuFEx) and strain-promoted azide-alkyne cycloaddition (SPAAC), are a part of emerging trends in click chemistry that expand the range of applications. Click chemistry has improved lead compound synthesis, made it easier to develop pharmacophore linkers, and produced bio isosteres to improve drug potency and metabolic stability in the drug discovery process. The method's role in creating cutting-edge treatments has also been highlighted by its contribution to the discovery of inhibitors for diseases like HIV, cancerous development, and bacterial infections. From early stage drug discovery to clinical development, click chemistry remains at the forefront of pharmaceutical analysis, highlighting its critical influence on ongoing drug development.

Research Journal of Pharmacy and Technology
AIMST University (MY)
Openalex Percentile: Top 91%
Click Chemistry and Applications
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Click chemistry in drug development recent trends and application — Kamini Vijeepallam, Murali Sundaram, et al. · Research Journal of Pharmacy and Technology (2025) | TGRS Research Map | TGRS