Antifungal agents : Novel fused pyrimidone and triazinone derivatives

L'innovation

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.

Ses bénéfices
Active on azole-susceptible and resistant strains (Candida spp., Aspergillus fumigatus )
No cytotoxic effect
Chemical properties for oral, transdermal or intravenous administration

Ses applications
Treatment or prevention of fungal infections
Second application : treatment or prevention of parasitic infectious due to Trypanosomatidae.

Stade de développement
IN VIVO - Preuve de concept

Laboratoire de recherche
EA 1155 - IICIMED

Équipe de recherche
DEPARTEMENT DE PARASITOLOGIE ET MYCOLOGIE MEDICALE

Propriété intellectuelle associée
WO : PCT/EP2015/067752 - filed on the 07-31-2015
WO - CA,EP,JP,US