Due to their ease of use including administration route and relative inocuity, the azole derivatives (such fluconazole, itraconazole, voriconazole, posaconazole) are widespread antifungal agents. However, their use as first intention has lead to resistance.
Besides azole anti-fungal agents, alternative classes include polyenes such as amphotericine B (Fingizone) and its lipidic forms, as well as the echinocandines. Hoever, these alternative antifungal agents are fenerally costly and not suitable for oral administation for treating systemic disorders.
We have developed new azole antifungal derivatives in particular compounds able to circumvent resistance phenomenons, such as those originating from mutations of the gene coding for their target (14a-demethylase, CYP51) and/or their efflux 20 by pumps of the CDR or MDR pumps.
These compounds present high antifungal activity on numerous azole resistant strains without side effect.
EA 1155 - IICIMED
DEPARTEMENT DE PARASITOLOGIE ET MYCOLOGIE MEDICALE
WO : PCT/EP2015/067752 - filed on the 07-31-2015
WO - CA,EP,JP,US