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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.

Herein, we reported the synthesis of nineteen novel 1,2,4-triazole derivatives including 1,3-diphenyl-2-(1H-1,2,4-triazol-1-yl) propan-1-ones (7a-e), 1-(1,3-diphenylpropan-2-yl)-1H-1,2,4-triazole (8a-c) and 1,4-diphenyl-2-(1H-1,2,4-triazol-1-yl) butane-1,4-diones (10a-k). The structures of these derivatives were confirmed by spectroscopic techniques like IR, 1H-NMR, Mass spectroscopy and Elemental analysis. The cytotoxic activities of the synthesized compounds were evaluated against three human cancer cell lines including MCF-7, Hela and A549 using MTT assay. Compounds 7d, 7e, 10a and 10d showed a promising cytotoxic activity lower than 12 μM against Hela cell line. The safety of these compounds was also, evaluated on MRC-5 as a normal cell line and relieved that most of the synthesized compounds have proper selectivity against normal and cytotoxic cancerous cell lines. Finally, molecular docking studies were also, done to understand the mechanism and binding modes of these derivatives in the binding pocket of aromatase enzyme as a possible target.

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