Metallo-β-lactamase inhibitory activity of 3-alkyloxy and 3-amino phthalic acid derivatives and their combination effect with carbapenem
作者:Yukiko Hiraiwa、Akihiro Morinaka、Takayoshi Fukushima、Toshiaki Kudo
DOI:10.1016/j.bmc.2013.07.006
日期:2013.9
3-Alkyloxy and 3-amino phthalic acid derivatives were found to have metallo-β-lactamase inhibitory activity. Among them, 3-amino phthalic acid derivatives showed both potent activity against metallo-β-lactamase, IMP-1 inhibitory activity and a strong combination effect with biapenem (BIPM), carbapenem antibiotic. In particular, the 4′-hydroxy-piperidine derivative showed strong IMP-1 inhibitory activity
发现3-烷氧基和3-氨基邻苯二甲酸衍生物具有金属-β-内酰胺酶抑制活性。其中,3-氨基邻苯二甲酸衍生物既显示出对金属β-内酰胺酶的有效活性,又显示出IMP-1的抑制活性,并且与碳青霉烯类抗生素比阿培南(BIPM)具有很强的联合作用。特别地,4'-羟基-哌啶衍生物显示出强的IMP-1抑制活性以及与各种抗生素的组合作用。