CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS

摘要

The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m′-X]p-L; (iii) AFA-[X-(L)n′]q; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.

主权项

1. A conjugate-based antifungal or antibacterial prodrug of formula:
(i) (AFA)m-X-(L)n, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; and n ranges from 2 to 10; (ii) [(AFA)m′-X]p-L, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m′ is 1 to 10; and p is 1 to 10; (iii) AFA-[X-(L)n′]q, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; X is a linker; and m″ is 1 to 10.