Candida albicansis the most common fungal pathogen associated with human opportunistic infections. Invasive infections caused by C. albicansare becoming increasingly serious. However, with the rising incidence of fungal infection, many fungi are resistant to commonly used drugs. Therefore, there is an urgent need for exploring new anti-fungal drugs that fungi are not resistant to. A series of novel azole derivatives linked to indole/indoline moieties were prepared, and in vitroantifungal activity evaluated. All compounds combined with FLC showed excellent activity against drug-resistant C. albicanswith low toxicity. A preliminary mechanistic study indicated that S1combined with FLC could inhibit the formation of C. albicansbiofilms as well as destroy the integrity of cell-membrane structure and mitochondrial function. S1could be considered a new fungal agent for further study.