Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus.

Autor: Sweeney NL; Department of Pharmaceutical Sciences, Concordia University Wisconsin, 12800 N Lake Shore Dr, Mequon, WI 53097, USA. noreena.sweeney@cuw.edu., Lipker L; Department of Microbiology, University of Wisconsin-La Crosse, La Crosse, WI 54601, USA. lipker.laur@uwlax.edu., Hanson AM; Department of Pharmaceutical Sciences, Concordia University Wisconsin, 12800 N Lake Shore Dr, Mequon, WI 53097, USA. alicia.schultz@cuw.edu., Bohl CJ; Department of Pharmaceutical Sciences, Concordia University Wisconsin, 12800 N Lake Shore Dr, Mequon, WI 53097, USA. chris.bohl@cuw.edu., Engel KE; Department of Microbiology, University of Wisconsin-La Crosse, La Crosse, WI 54601, USA. katieengel92@gmail.com., Kalous KS; Department of Biochemistry, Medical College of Wisconsin, Wauwatosa, WI 53226, USA. kekalous@mcw.edu., Stemper ME; Marshfield Clinic Research Foundation, Marshfield, WI 54449, USA. stemper.mary@marshfieldclinic.org., Sem DS; Department of Pharmaceutical Sciences, Concordia University Wisconsin, 12800 N Lake Shore Dr, Mequon, WI 53097, USA. Daniel.Sem@cuw.edu., Schwan WR; Department of Microbiology, University of Wisconsin-La Crosse, La Crosse, WI 54601, USA. wschwan@uwlax.edu.
Jazyk: angličtina
Zdroj: Antibiotics (Basel, Switzerland) [Antibiotics (Basel)] 2017 Jan 28; Vol. 6 (1). Date of Electronic Publication: 2017 Jan 28.
DOI: 10.3390/antibiotics6010004
Abstrakt: The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Staphylococcus aureus . Initially, the project was focused on discovering small molecules that may have antibacterial properties targeting the Mycobacterium tuberculosis thioredoxin reductase. This led to the discovery of a pyrazolone scaffold-containing compound series that showed bactericidal capability against S. aureus strains, including drug-resistant clinical isolates. The findings support continued development of the pyrazolone compounds as potential anti- S. aureus antibiotics.
Databáze: MEDLINE
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