| abstract |
The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y 1 ) m —Ar 1 (X 1 )—C(=O)VAr 2 (X 2 )−(Y 2 ) p (I), wherein V designates —CH 2 —CH 2 —, —CH═CH— or —C≡C—; Ar 1 and Ar 2 independently are aryl and heteroaryl; m=0, 1, 2, p=0, 1, 2, m+p>0; each Y 1 and Y 2 independently is -Z—N + (R 1 )(R 2 )R 4 Q − (A); —NR 3 -Z—N + (R 1 )(R 2 )R 4 Q − (B), or —O-Z—N + (R 1 )(R 2 )R 4 Q − (C), R 1 , R 2 , R 3 , R 4 , X 1 , X 2 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. |