1,2,4-Triazole: A Privileged Scaffold for the Development of Potent Antifungal Agents - A Brief Review

Abstract

<jats:sec> <jats:title>:</jats:title> <jats:p>Over the past decades, a dramatically tremendous rise in invasive fungal infection diseases attributed to the yeast Candida albicans in immunocompromised individuals poses a serious challenging issue. Another alarming concern is the emergence of multi-drug resistant pathogens to the existing medicines due to their overuse and misuse. 25% to 55% mortality, caused by the invasive infection, was recently reported. Despite a large variety of drugs available to treating invasive candidiasis, only two of them containing a 1,2,4-triazole core, fluconazole and itraconazole, are efficient for the infection therapy induced by fungal Candida species. Moreover, the long-term therapy associated with the azole medications has led to an increase in azole resistance and to high risk of toxicity. Despite numerous outstanding achievements in antifungal drug discovery, the development of novel potent antifungal agents in view to develop more potent and safer fungicides and to overcome the resistance problem associated with the actual drugs is becoming the main focus point for medicinal chemists. Thus, the purpose of the present review is to outline the progresses of the last decade in medicinal chemistry research devoted to the 1,2,4-triazole-based derivatives as potential antifungal agents. The structure activity relationship of these compounds is also discussed.</jats:p> </jats:sec>

Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

“…This is evi-denced by the use of drugs Itraconazole, Fluconazole in the world medical practice. The works of scientists [11][12][13][14][15][16][17][18][19][20] confirm this. Systematizing the literature, we can conclude that the substituents adamantane, 5-amino-2-hydroxybenzoate, 4-fluoro-2-phenoxyphenyl, 2-bromophenyl and hydroxybenzylidene fragment in the 5 position of the heterocyclic system of 1,2,4-triazole lead to an increase in antifungal action.…”

Design, Synthesis, in vitro and in silico Characterization of 2‐Quinolone‐L‐alaninate‐1,2,3‐triazoles as Antimicrobial Agents

“…[ 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 ] One useful strategy has been to create hybrid molecules [26] using two different pharmacophoric moieties with antimicrobial effects. 2‐Quinolones could be combined with, for example, the privileged scaffolds of 1,2,3‐ or 1,2,4‐triazoles[ 27 , 28 , 29 ] that have both been widely applied not only in medicinal chemistry[ 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 ] but also in material science. [ 39 , 40 ]…”

3-Phenyl-4-(prop-2-en-1-yl)-5-[(prop-2-en-1-yl)sulfanyl]-4H-1,2,4-triazole

“…Chemists are interested in 1,2,4-triazole derivatives mainly because of their wide range of pharmacological activities, such as antifungal, herbicidal, antiviral and anticancer activities, as well as catalase inhibitors. Some drugs that are clinically used for the treatment of various diseases are based on them [1][2][3][4][5][6][7][8]. Commercial fungicides also contain triazoles [9].…”