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Antibiotics 2017, 6(1), 4; doi:10.3390/antibiotics6010004

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

1
Department of Pharmaceutical Sciences, Concordia University Wisconsin, 12800 N Lake Shore Dr, Mequon, WI 53097, USA
2
Department of Microbiology, University of Wisconsin-La Crosse, La Crosse, WI 54601, USA
3
Department of Biochemistry, Medical College of Wisconsin, Wauwatosa, WI 53226, USA
4
Marshfield Clinic Research Foundation, Marshfield, WI 54449, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Christopher C. Butler
Received: 17 November 2016 / Revised: 19 January 2017 / Accepted: 23 January 2017 / Published: 28 January 2017
(This article belongs to the Special Issue Discover New Antibiotics 2016)
View Full-Text   |   Download PDF [3119 KB, uploaded 6 February 2017]   |  

Abstract

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. View Full-Text
Keywords: thioredoxin reductase; antibiotic target; molecular docking; enzyme inhibitor; MRSA; pyrazolones thioredoxin reductase; antibiotic target; molecular docking; enzyme inhibitor; MRSA; pyrazolones
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Sweeney, N.L.; Lipker, L.; Hanson, A.M.; Bohl, C.J.; Engel, K.E.; Kalous, K.S.; Stemper, M.E.; Sem, D.S.; Schwan, W.R. Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus. Antibiotics 2017, 6, 4.

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