Development of carbapenem-based fluorogenic probes for the clinical screening of carbapenemase-producing bacteria

Title
Development of carbapenem-based fluorogenic probes for the clinical screening of carbapenemase-producing bacteria
Authors
추현아김주현Yihoon KImAhmed Z. AbdelazemHak Joong KimJung Ok KimYeon-Joon ParkSun-Joon MinHoon Seok Kim
Keywords
Carbapenems; carbapenemase-producing bacteria; linker; fluorescence; probes
Issue Date
2020-01
Publisher
Bioorganic chemistry
Citation
VOL 94-14
Abstract
This report describes the synthesis of a library of fluorogenic carbapenemase substrates consisting of carbapenem derivatives, fluorescence dyes, and active cleavable linkers and their evaluation for specifically detecting carbapenemase-producing organisms (CPOs). We synthesized a series of compounds having three different types of linkers such as benzyl ether, carbamate, and amine using hydroxymethyl carbapenem 7a and hydroxyallyl carbapenem 7b as key intermediates. Probe 1b exhibited high stability and a prompt turn-on fluorescence signal upon hydrolysis by carbapenemases. In particular, the screening of clinical samples indicated that the probe 1b exhibited excellent selectivity to the CPOs over other β-lactamases or non-carbapenemase producing bacteria, which may be of clinical use for the rapid and accurate detection of CPOs for timely diagnosis and treatment.
URI
http://pubs.kist.re.kr/handle/201004/71015
ISSN
0045-2068
Appears in Collections:
KIST Publication > Article
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