Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor

…, C Wu, ZJ Ni, J Trias, RJ White, Z Yuan - Biochemistry, 2000 - ACS Publications
Peptide deformylase (PDF) is essential in prokaryotes and absent in mammalian cells, thus
making it an attractive target for the discovery of novel antibiotics. We have identified …

New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile

MF Gordeev, ZY Yuan - Journal of medicinal chemistry, 2014 - ACS Publications
Oxazolidinones comprise an important class of antibacterial protein synthesis inhibitors.
Myelosuppression and monoamine oxidase inhibition (MAOI) are key independent causes for …

N-Alkyl Urea Hydroxamic Acids as a New Class of Peptide Deformylase Inhibitors with Antibacterial Activity

…, DV Patel, B Weidmann, RJ White, Z Yuan - Antimicrobial agents …, 2002 - Am Soc Microbiol
Peptide deformylase (PDF) is a prokaryotic metalloenzyme that is essential for bacterial
growth and is a new target for the development of antibacterial agents. All previously reported …

Deformylase as a novel antibacterial target

Z Yuan, J Trias, RJ White - Drug Discovery Today, 2001 - Elsevier
Bacterial genomics has revealed a plethora of previously unknown targets of potential use
in the discovery of novel antibacterial drugs. However, so far little has emerged from this …

Peptide Deformylase in Staphylococcus aureus: Resistance to Inhibition Is Mediated by Mutations in the Formyltransferase Gene

…, DC Young, W Wang, D Chen, Z Yuan… - Antimicrobial agents …, 2000 - Am Soc Microbiol
Peptide deformylase, a bacterial enzyme, represents a novel target for antibiotic discovery.
Two deformylase homologs, defA and defB, were identified inStaphylococcus aureus. The …

A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft …

X Zhao, H Huang, H Yuan, Z Yuan… - Journal of Antimicrobial …, 2022 - academic.oup.com
Objectives Contezolid is a novel oxazolidinone antibacterial agent for managing infections
caused by aerobic and anaerobic Gram-positive bacteria including methicillin-resistant strains…

Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies

…, H Wang, Q Dai, C Liu, X Wang, Z Yuan… - ACS Medicinal …, 2022 - ACS Publications
New oral antibiotic contezolid (CZD) is effective against Gram-positive infections but unsuitable
for intravenous (IV) administration due to its modest solubility. To address the medical …

Metabolism of MRX-I, a novel antibacterial oxazolidinone, in humans: the oxidative ring opening of 2, 3-dihydropyridin-4-one catalyzed by non-P450 enzymes

J Meng, D Zhong, L Li, Z Yuan, H Yuan, C Xie… - Drug metabolism and …, 2015 - ASPET
MRX-I is an analog of linezolid containing a 2,3-dihydropyridin-4-one (DHPO) ring rather
than a morpholine ring. Our objectives were to characterize the major metabolic pathways of …

Targeting metalloenzymes: a strategy that works

RJ White, PS Margolis, J Trias, Z Yuan - Current Opinion in Pharmacology, 2003 - Elsevier
Faced with a wealth of antibacterial drug discovery targets as a result of bacterial genomics,
we need to carefully select which ones to work with. Choosing bacterial metalloenzymes is …

A dual culture assay for detection of antimicrobial activity

…, B Ruhland, PJ Schatz, Z Yuan - Journal of …, 1996 - journals.sagepub.com
Combinatorial chemistry has opened a new realm of chemical diversity in the search for useful
therapeutics as well as the ability to generate chemical libraries of hundreds of thousands …