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http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/2141| Title: | Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors |
| Authors: | PARDESHI, KUNDANSINGH A. MALWAL, SATISH R. Banerjee, Ankit Lahiri, Surobhi Rangarajan, Radha CHAKRAPANI, HARINATH Dept. of Chemistry |
| Keywords: | MRSA Sulfur dioxide Thiol Reactive oxygen species Drug resistance 2015 |
| Issue Date: | Jul-2015 |
| Publisher: | Elsevier B.V. |
| Citation: | Bioorganic and Medicinal Chemistry Letters, 25(13), 2694-2697. |
| Abstract: | Drug resistant infections are becoming common worldwide and new strategies for drug development are necessary. Here, we report the synthesis and evaluation of 2,4-dinitrophenylsulfonamides, which are donors of sulfur dioxide (SO2), a reactive sulfur species, as methicillin-resistant Staphylococcus aureus (MRSA) inhibitors. N-(3-Methoxyphenyl)-2,4-dinitro-N-(prop-2-yn-1-yl)benzenesulfonamide (5e) was found to have excellent in vitro MRSA inhibitory potency. This compound is cell permeable and treatment of MRSA cells with 5e depleted intracellular thiols and enhanced oxidative species both results consistent with a mechanism involving thiol activation to produce SO2. |
| URI: | http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/2141 https://doi.org/10.1016/j.bmcl.2015.04.046 |
| ISSN: | 0960-894X 1464-3405 |
| Appears in Collections: | JOURNAL ARTICLES |
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