Quaternary Amino-Function Chalcones

摘要

The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y¹)_m-Ar¹(X¹)-C(=O)VAr²(X²)-(Y²)_p (I), wherein V designates -CH₂-CH₂-, -CH-CH- or -C≡C-; Ar¹ and Ar² independently are aryl and heteroaryl; m=0, 1, 2, p=0, 1, 2, m+p>0; each Y¹ and Y² independently is -Z-N⁺(R¹)(R²)R⁴ Q^- (A); -NR³-Z-N⁺(R¹)(R²)R⁴ Q^- (B), or -O-Z-N⁺(R¹)(R²)R⁴ Q^- (C), R¹, R², R³, R⁴, X¹, X² are substituents, and Q^- is an anion. The present invention also relates to the compounds for use as pharmaceutically active agents, in particular against bacterial infections (such as Gram-negative and Gram-positive bacteria, including antibiotic-sensitive or resistant strains), and in the medical treatment of bacterial infections in mammals.