Azole Derivatives: Recent Advances as Potent Antibacterial and Antifungal Agents

Abstract

Background: Azoles are the famous and widespread scaffold in the pharmaceutical industry through wide range of activities, high efficacy, and good tolerability and oral availability. Furthermore, azole derivatives have engrossed attentiveness as potent antimicrobial agents. Introduction: The purpose of this review is to execute an overview of the pharmacological aspects of the main scaffolds of azoles, including imidazole, benzimidazole, triazole and tetrazole which possessed antimicrobial activity from 2016 to 2020 as well as all of our publication in this field. In addition, we discussed the relationship between the structure and activity and molecular docking studies of the azole derivatives to provide key features and useful information for the synthesis of novel azole compounds with desirable biological activities. The presented structures in this review have been tested against several bacteria and fungi such that E. coli and C. albicans were common in all of these studies. Results: The comparison of reported MIC showed that fluconazole base structures were the most active ones as antifungal agents and triazole derivatives bearing nitrophenyl and coumarin moieties had the most antibacterial activity. Conclusion: Triazole and imidazole scaffolds are more important in the design of antimicrobial compounds than other azole derivatives like benzimidazole or tetrazole. All the most active compounds fulfilled the Lipinski rules.

Antimicrobial Properties of Azole Functional Silica Nanocomposites

“…Tejera et al [53] similarly tested the antimicrobial activity of thiazolium and triazolium side chain polymethacrylates on bacterial species. Moreover, azole derivatives have been used in various studies for different purposes and find a wide application area due to their antibacterial [54][55][56] and antifungal [56] properties. In contrast to these studies that focus on azole derivatized core nanoparticles, in our current study functionalized nanocomposites were decorated with azole derivatives on their surface.…”

Synthesis and in silico inhibitory action studies of azo-anchored imidazo[4,5-b]indole scaffolds against the COVID-19 main protease (Mpro)

“…Intriguingly, the nitrogen-embracing heterocyclic framework is the most prevalent structural motifs found in pharmaceutical chemistry as biologically active synthetic equivalents and natural products 23 – 25 . Subsequently, the development of imidazole-based therapeutic agents has acquired significant attention on account of their synthetic and effective biological significance.…”

Organocatalytic Atroposelective Construction of Pentatomic Heterobiaryl Diamines through Arylation of 5-Aminoisoxazoles with Azonaphthalenes

“…Azoles are essential components of five-membered nitrogen-containing heterocycles and exhibit numerous biological activities, including insecticidal, antimicrobial, antitumor, antifungal, etc . Owing to the importance of azoles in drug discovery, the construction of chiral skeletons containing azoles is of great significance and interest.…”