| 摘要 |
<p>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 -CH2-CH2-, -CH=CH-or -C=C; Ar<1> and Ar<2> independently are aryl and heteroary.; m=0, 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 sue 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.</p> |
