Synthesis of Imidazole-Based Medicinal Molecules Utilizing the van Leusen Imidazole Synthesis.

Xunan Zheng,Zhengning Ma,Dawei Zhang

doi:10.3390/ph13030037

Xunan Zheng, Zhengning Ma + Show 1 more

Open Access

https://doi.org/10.3390/ph13030037

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Abstract

Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activities, and are widely researched and applied by pharmaceutical companies for drug discovery. The van Leusen reaction based on tosylmethylisocyanides (TosMICs) is one of the most appropriate strategies to synthetize imidazole-based medicinal molecules, which has been increasingly developed on account of its advantages. In this review, we summarize the recent developments of the chemical synthesis and bioactivity of imidazole-containing medicinal small molecules, utilizing the van Leusen imidazole synthesis from 1977.

Highlights

Imidazole ring, which is widely found in natural products and medical molecules, is one of the most prominent, five-membered, nitrogen-containing, heterocyclic scaffolds
Imidazole-based heterocyclic compounds, which possess a vital position in medicinal chemistry, have been playing a central role in the treatment of numerous types of diseases, and new derivatives for medicinal use are being energetically developed worldwide [1,2,3,4,5]
Due to the peculiar structural characteristic of imidazole scaffold with a worthy electron-rich feature, it is advantageous for imidazole groups to combine with various receptors and enzymes in biological systems, through diverse weak interactions, thereby showing a variety of biological activities

Summary

Introduction

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Conclusions