During the past two decades，the life threatening infections caused by pathogenic fungi have become increasingly common，especially in individuals with immunocompromised hosts，such as patients undergoing anticancer chemotherapy or organ transplants and patients with AIDS. Clinically，candidosis，aspergillosis and cryptococcosis are three major fungal infections in immunocompromised individuals. Moreover，dermatomycoses，such as toenails and tinea pedis，are among the most widespread human superficial and cutaneous fungal infections. However，the current antifungal therapy suffers from drug related toxicity，severe drug resistance，nonoptimal pharmacokinetics and serious drug-drug interactions. Therefore，there is an emergent need to develop novel antifungal drugs with higher efficiency，broaderspectrum and lower toxicity.