Compounds made up by the grafting of amino acid and triazole with indole moiety were synthesized and investigated for antifungal activities whereby one of the compounds gave highly promising results. Although the compound has high MIC80 value in liquid medium, it shows significant antifungal activity against Candida albicans in solid plate assays. The compound is found to target chitin in the cell wall and lanosterol 14α-demethylase of the ergosterol biosynthesis pathway, respectively. The inhibitory effect of the compound becomes more pronounced in combination with azoles and CFW. The compound is also found to significantly affect chitin levels, cell morphology and cell viability in combination with ketoconazole.