作者
SATISH R MALWAL, Surobhi Lahiri, HARINATH CHAKRAPANI, Ankit Banerjee, KUNDANSINGH A PARDESHI, Radha Rangarajan
发表日期
2015
出版商
Elsevier BV
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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SR MALWAL, S Lahiri, H CHAKRAPANI, A Banerjee… - 2015