Title:Azole Derivatives: Recent Advances as Potent Antibacterial and Antifungal
Agents
Volume: 30
Issue: 2
关键词:
唑,抗菌,分子对接,SAR, MIC, Lipinski规则
摘要:
Background: Azoles are the famous and widespread scaffold in the pharmaceutical
industry due to their wide range of activities, high efficacy, good tolerability,
and oral availability. Furthermore, azole derivatives have attracted attention as potent antimicrobial
agents.
Introduction: The purpose of this review is to provide an overview of pharmacological
aspects of the main scaffolds of azoles, including imidazole, benzimidazole, triazole, and
tetrazole, which possess antimicrobial activity, reported from 2016 to 2020, as well as all
of our publication in this field. In addition, we discuss the relationship between structure
and activity and molecular docking studies of the azole derivatives to provide critical features
and valuable 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 as E. coli and C. albicans, which have been common in all
of these studies.
Results: A comparison of the reported MIC for tested compounds showed fluconazole
base structures as the most active antifungal agents, and triazole derivatives bearing nitrophenyl
and coumarin moieties to have the most dominant antibacterial activity.
Conclusion: Triazole and imidazole scaffolds are more important for designing antimicrobial
compounds than other azole derivatives, like benzimidazole or tetrazole. All the
most active compounds were observed to fulfill the Lipinski rule.