Fluconazole-cox inhibitor hybrids: a dual-acting class of antifungal azoles
AssigneeRamot at Tel-Aviv University Ltd.
InventorsMICHA FRIDMAN, REBECA ELIAS, PALLABITA BASU
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Abstract
A novel dual-acting class of antifungal compound synthesized by linking an azole pharmacophore to a COX inhibitor to form a hybrid molecule. A method of making the antifungal compound by preparing a mixture of an azide-functionalized pharmacophore, subjecting the azide-functionalized pharmacophore to catalytic hydrogenation to obtain an amine-functionalized azole pharmacophore, and coupling a COX inhibitor to the amine-functionalized azole pharmacophore. A method for treating fungal infection in plants and animals comprising administering the antifungal compound.
Claims24
An antifungal compound, an (R) enantiomer thereof, an (S) enantiomer thereof, a diastereomer thereof, a racemate thereof, or a salt thereof, comprising:
- an azole pharmacophore coupled to an Ru moiety via a link;
- wherein Ru is a COX inhibitor coupled to the azole pharmacophore via an amide bond between a primary amine of the azole pharmacophore and a carboxylic acid of the COX inhibitor;
- and
- wherein the antifungal compound is according to Formula (I),
(canceled)
9-12. (canceled)
(canceled)
27-39. (canceled)
Dependencies are inferred from the claim text.