The synthesis of 7-substituted-3-dinitrostyryl cephalosporins and their ability for detecting extended spectrum beta-lactamases (ESBLs).
We synthesized 7-substituted-3-(2,4-dinitrostyryl)cephalosporin derivatives which were Nitrocefin analogs, for detecting extended spectrum beta-lactamase (ESBL) specifically. HMRZ-86 which has carboxypropyloxyimino group on 7-aminothiazolacetamide substituent were not hydrolyzed by class A, C and D beta-lactamases, but it was hydrolyzed by ESBL and metallo beta-lactamase (class B), then its color changed from yellow to red. The hydrolysis of metallo beta-lactamase was inhibited by adding sodium mercapto acetic acid (SMA). Therefore HMRZ-86 is a useful chromogenic agent to detect ESBL specifically.
Hanaki
Hideaki
H
Research Center for Anti-infective Drugs, Kitasato Institure, Minato-ku, Tokyo 108-8641, Japan.
Yamazaki
Hiroaki
H
Harada
Hidenori
H
Kubo
Ryoichi
R
Kobayashi
Takayoshi
T
Atsuda
Koichiro
K
Sunakawa
Keisuke
K
D002511:Cephalosporins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003116:Color; D006868:Hydrolysis / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D001618:beta-Lactamases / Q000187:drug effects*
D002511:Cephalosporins; C487639:HMRZ 86; D001618:beta-Lactamases