Medicinal attributes of 1,2,3-triazoles: Current developments.

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Pharmacology

Background:

• 1,2,3-Triazoles represent a critical five-membered heterocyclic scaffold with diverse biological activities.
• Their synthesis is efficiently achieved through click chemistry, yielding multigram quantities under ambient conditions.
• The pharmacological scope of triazoles has garnered significant global research interest.

Purpose of the Study:

• To review current synthetic methodologies for 1,2,3-triazoles.
• To summarize the medicinal significance of triazole architectures as lead structures in drug discovery.
• To highlight advancements in the medicinal applications of triazoles between 2008 and 2016.

Main Methods:

• Literature review of synthetic approaches for 1,2,3-triazoles.
• Analysis of published data on the biological activities and medicinal applications of triazole derivatives.
• Focus on drug candidates in clinical trials, including COX-1/COX-2 inhibitors, HIV protease inhibitors, and CB1 receptor antagonists.

Main Results:

• Click chemistry provides a robust and scalable route to 1,2,3-triazoles.
• Triazole-based compounds exhibit a wide range of pharmacological activities.
• Several triazole derivatives are progressing through clinical trials for various therapeutic indications.

Conclusions:

• 1,2,3-Triazoles are privileged structures in medicinal chemistry due to their synthetic accessibility and broad biological relevance.
• Continued research into triazole synthesis and medicinal applications is expected to yield new therapeutic agents.
• The period 2008-2016 saw significant progress in leveraging triazoles for drug discovery.