3-烷氧基和 3-氨基邻苯二甲酸衍生物的金属-β-内酰胺酶抑制活性及其与碳青霉烯的联合效应。
Metallo-β-lactamase inhibitory activity of 3-alkyloxy and 3-amino phthalic acid derivatives and their combination effect with carbapenem.
机构信息
Pharmaceutical Research Center, Meiji Seika Pharma, Co., Ltd, Kohoku-ku, Yokohama, Japan.
出版信息
Bioorg Med Chem. 2013 Sep 15;21(18):5841-50. doi: 10.1016/j.bmc.2013.07.006. Epub 2013 Jul 18.
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 and a combination effect with various antibiotics.
3-烷氧基和 3-氨基邻苯二甲酸衍生物被发现具有金属β-内酰胺酶抑制活性。其中，3-氨基邻苯二甲酸衍生物不仅对金属β-内酰胺酶具有很强的抑制活性，对 IMP-1 也有抑制作用，并且与碳青霉烯类抗生素比阿培南（BIPM）具有很强的协同作用。特别是 4'-羟基哌啶衍生物对 IMP-1 具有很强的抑制活性，并与各种抗生素具有协同作用。
Zotero 插件