A phthalic acid derivative represented by the general formula (1) has an inhibitory activity on metallo-β-lactamase. Therefore, when used in combination with a β-lactam antibiotic, the derivative can inhibit the deactivation of the β-lactam antibiotic against a bacterium capable of producing ...
Name Metallo-β-lactamase-IN-9 Description Metallo-β-lactamase-IN-9 (Compound 23) serves as a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), exhibiting inhibition constants (IC50) of 35 nM for NDM-1, 269 nM for VIM-1, and 369 nM for IMP-1 [1]. In vivo 金属β-内酰胺酶...
4-Butyl-3-methylphthalic acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted phthalic acids afforded 3-phenylphthalic acid derivatives as potent IMP-1 inhibitors. On the other hand, 3-substi
metallo-beta-lactamasescoring functionMOLECULAR-FORCE FIELDFAVORABLE BINDING-SITESPROTEIN-LIGAND DOCKINGINCREMENTAL CONSTRUCTION ALGORITHMBROAD-SPECTRUM INHIBITORThe performance of the AutoDock, GOLD and FlexX docking programs was evaluated for docking of dicarboxylic acid inhibitors into metallo-beta-lactamases (...
inhibitor for New Delhi metallo-β-lactamase-1 and other metallo-β-lactamases classes, so metallo-β-lactamases inhibitor drugs became an urgent need. In this study, multi-steps virtual screening was done over the NPASS database with 35,032 natural compounds. At first Captopril was extracted ...
T. et al. ANT2681: SAR studies leading to the identification of a metallo-β-lactamase inhibitor with potential for clinical use in combination with meropenem for the treatment of infections caused by NDM-producing Enterobacteriaceae. ACS Infect. Dis. 6, 2419–2430 (2020). Article CAS PubMed ...
aureus—resistant to methicillin and all beta lactums (penicillins, cephalosporins) with or without beta-lactamase inhibitor combination, macrolides and carbapenems. But sensitive to vancomycin. • Vancomycin-resistant S. aureus—methicillin-resistant S. aureus has been reported to h...
NOTA: a potent metallo-beta-lactamase inhibitor Metallo-β-lactamaseInhibitorAzolylthioacetamidesIn an effort to develop new inhibitors of metallo--lactamases (MLs), twenty-eight azolylthioacetamides were ... AM Somboro,D Tiwari,LA Bester,... - 《Journal of Antimicrobial Chemotherapy》 被引量: ...
The resistance of bacteria to the normally lethal action of beta-lactam antibiotics is largely due to the production of beta-lactamases that catalyze the hydrolysis of the beta-lactam. One class of these enzymes is a zinc-dependent metallo-beta-lactamase for which there are no clinically available...
Shlaes, D. M., “New beta-lactam-beta-lactamase inhibitor combinations in clinical development,” Ann. NY Acad. Sci., 2013, 1277:105-114. Yigit et al., “Novel carbapenem-hydrolyzing beta-lactamase, KPC-1, from a carbapenem-resistant strain of Klebsiella pneumoniae,” Antimicrob. Agents nd...