121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-653
Subject Synthetic studies towards the development of fluorogenic probes for the detection of carbapenemase producing bacteria
Authors Ahmed Zakaria Abdelazem, Sun-Joon Min1,*
Dept of Chemical & Molecular Engineering/Applied Chemistry, Hanyang University, Korea
1Dept of Chemical & Molecular Eng/Applied Chemistry, Hanyang University, Korea
Abstract Antibiotic resistance has become a major challenge to the public health worldwide. Carbapenems, such as imipenem, doripenem, and meropenem, are considered as the antibiotics of last option for the treatment of severe infections due to their broad spectrum of activity against both Gram positive and Gram-negative bacterial pathogens. However, carbapenem-resistant bacteria have become increasingly widespread throughout the world in the last years. The major mechanism of resistance to carbapenem among Gram-negative bacteria is associated with the acquisition or expression of carbapenemases. Carbapenemases are a group of specific β-lactamases that have the ability to hydrolyze carbapenems, as well as nearly all other β-lactam antibiotics. To prevent the spread of carbapenem-resistant bacteria; early detection is highly needed. Carbapenemases have been classified into two major groups: (i) serine carbapenemases, which possess a serine residue active-site as a nucleophile to cleave the β-lactam ring; and (ii) metallo-β-lactamases, which require a Zn2+–OH for nucleophilic attack on the β-lactam bond. In both cases, the carbapenemase mediated hydrolysis is a crucial mechanism of the carbapenem-resistance. Thus, substrate-based chemical probes would be a rational approach to detect the carbapenemase producing organisms, which are resistant to the carbapenm class of antibiotics. Herein, we would like to highlight some synthetic studies aimed at the development of substrate-based fluorogenic probes for the detection of carbapenemase producing bacteria.
E-mail aznagi2003@gmail.com