作者
Kundansingh A Pardeshi, Satish R Malwal, Ankita Banerjee, Surobhi Lahiri, Radha Rangarajan, Harinath Chakrapani
发表日期
2015/7/1
期刊
Bioorganic & Medicinal Chemistry Letters
卷号
25
期号
13
页码范围
2694-2697
出版商
Pergamon
简介
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.
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KA Pardeshi, SR Malwal, A Banerjee, S Lahiri… - Bioorganic & Medicinal Chemistry Letters, 2015