Current Advances in the Synthesis and Biological Evaluation of Pharmacologically Relevant 1,2,4,5-Tetrasubstituted-1H-Imidazole Derivatives

Author(s): Renzo Rossi*, Maurizio Ciofalo*

Journal Name: Current Organic Chemistry

Volume 23 , Issue 19 , 2019

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Graphical Abstract:


Abstract:

In recent years, the synthesis and evaluation of the biological properties of 1,2,4,5-tetrasubstituted-1H-imidazole derivatives have been the subject of a large number of studies by academia and industry. In these studies it has been shown that this large and highly differentiated class of heteroarene derivatives includes high valuable compounds having important biological and pharmacological properties such as antibacterial, antifungal, anthelmintic, anti-inflammatory, anticancer, antiviral, antihypertensive, cholesterol-lowering, antifibrotic, antiuricemic, antidiabetic, antileishmanial and antiulcer activities.

The present review with 411 references, in which we focused on the literature data published mainly from 2011 to 2017, aims to update the readers on the recent developments on the synthesis and biological evaluation of pharmacologically relevant 1,2,4,5-tetrasubstituted-1H-imidazole derivatives with an emphasis on their different molecular targets and their potential use as drugs to treat various types of diseases. Reference was also made to substantial literature data acquired before 2011 in this burgeoning research area.

Keywords: 1H-Imidazoles, drugs, inhibitors, antibacterial agents, antifungals, antivirals, anti-inflammatory agents, anticancer agents, antihypertensive agents, antiobesity agents, antileishmanial agents, synthesis, review.

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