Mutations decreasing LYS228 susceptibility occurred in ramR and cpxA (Klebsiella pneumoniae) and baeS (E. These frequencies compared favorably to those obtained with meropenem and tigecycline. LYS228 MICs were ≤ 2 μg/mL against all mutants. At 4X the MIC, mutants were selected from two of twelve strains at frequencies of 1.8x10-7 and 4.2x10-9. No single-step mutants were selected from twelve Enterobacteriaceae strains expressing different classes of β-lactamases at 8X the minimum inhibitory concentration (MIC) of LYS228 (frequency <2.5x10-9). coli cells to LYS228 caused filamentation, consistent with cell division defects resulting from inhibition of PBP3. coli PBP3, with weaker binding to PBP1a and PBP1b. A gel-based PBP binding assay showed that LYS228 bound mainly to E. LYS228 bound purified Escherichia coli penicillin binding protein 3 (PBP3) similarly to ATM (k2/Kd = 367504 s-1M-29 s-1M-1, respectively) according to stopped-flow fluorimetry. The novel monobactam LYS228 is stable to MBLs and most SBLs. However, the clinically used monobactam aztreonam lacks stability to serine β-lactamases (SBLs) that are often co-expressed with MBLs. Glycosyltransferases and Transpeptidases/Penicillin-Binding Proteins: Valuable Targets for New Antibacterials.The monobactam chemical scaffold is attractive for the development of new agents to treat infections caused by drug-resistant Gram-negative bacteria since it is stable to metallo-β-lactamases (MBLs). Microbial siderophore-based iron assimilation and therapeutic applications. Angewandte Chemie International Edition 2016, 55 Antibiotikaresistenzen gezielt überwinden. Targeting human pathogenic bacteria by siderophores: A proteomics review. European Journal of Medicinal Chemistry 2018, 151, 98-109. Design, synthesis and biological evaluation of C(4) substituted monobactams as antibacterial agents against multidrug-resistant Gram-negative bacteria. Qunhuan Kou, Ting Wang, Feng Zou, Shuhua Zhang, Qian Chen, Yushe Yang.Antimicrobial Agents and Chemotherapy 2019, 64 Influence of the α-Methoxy Group on the Reaction of Temocillin with The Role of Iron and Siderophores in Infection, and the Development of Siderophore Antibiotics. Synthesis and antibacterial evaluation against resistant Gram-negative bacteria of monobactams bearing various substituents on oxime residue. Zhi–Wen Li, Xi Lu, Yan–Xiang Wang, Xin–Xin Hu, Hai–Gen Fu, Li–Mei Gao, Xue–Fu You, Sheng Tang, Dan–Qing Song.Antimicrobial Agents and Chemotherapy 2020, 64 Structural Insights into Ceftobiprole Inhibition of Pseudomonas aeruginosa Penicillin-Binding Protein 3. Papp-Wallace, Jacob Wyatt, Eric Desarbre, Robert A. Vijay Kumar, Christie Tang, Christopher R.A Glance on the Role of Bacterial Siderophore from the Perspectives of Medical and Biotechnological Approaches. Manaf AlMatar, Osman Albarri, Essam A.Medicinal Chemistry of β‐Lactam Antibiotics. Rational design of a new antibiotic class for drug-resistant infections. Tanudra, Jing Zhang, Janelle Comita-Prevoir, Jan A. Sylvester, Satenig Guler, Ramkumar Iyer, Adam B. Discovery of Novel Pyridone-Conjugated Monosulfactams as Potent and Broad-Spectrum Antibiotics for Multidrug-Resistant Gram-Negative Infections. Liang Tan, Yunliang Tao, Ting Wang, Feng Zou, Shuhua Zhang, Qunhuan Kou, Ao Niu, Qian Chen, Wenjing Chu, Xiaoyan Chen, Haidong Wang, and Yushe Yang.This article is cited by 14 publications.
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