Over the past decades, a tremendous rise in invasive fungal infection diseases attributed to the yeast Candida albicans in immunocompromised individuals poses a seriously challenging issue. Another concern is the emergence of multi-drug resistant pathogens to the existing medicines due to their overuse and misuse. It was recently reported that 25-55% of the mortality rate is caused by invasive infection. Despite a large variety of drugs being available to treat invasive candidiasis, only two of them contain a 1,2,4-triazole core, namely Fluconazole and itraconazole, which are efficient in treating infection induced by fungal Candida species. Moreover, long-term therapy associated with azole medications has led to an increase in azole resistance as well as a high risk of toxicity. Despite numerous outstanding achievements in antifungal drug discovery, development of novel, safer and potent antifungal agents while overcoming the resistance problem associated with the current drugs is becoming the main focus of medicinal chemists. Therefore, this review outlines the breakthroughs in medicinal chemistry research regarding 1,2,4- triazole-based derivatives as potential antifungal agents in the past decade. In addition, the structureactivity relationship of these compounds is also discussed.