The present invention is directed to compounds which have been identified, as inhibitors of the expression of CDR1 (Cdr1p) and/or CDR2 (Cdr2p), both ABC-type plasma, membrane transporters, which are major contributor to antifungal therapy resistance. These compounds may be used in the treatment of fungal infections, especially Candida infections, either alone or in combination with azole antifungal agents such as fluconazole, itraconazole, miconazole, clotrimazole and the like. Often the inhibitor compounds described herein are useful for reversing the antifungal therapy resistance exhibited by the overexpression of CDR1 and/or CDR2 in strains of fungi, especially including Candida spp. Combination therapy and compositions for treating fungal infections, especially including azole resistant fungal infections represent important embodiments of the present invention.