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http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/1926| Title: | Bioreductively Activated Reactive Oxygen Species (ROS) Generators as MRSA Inhibitors |
| Authors: | KHODADE, VINAYAK S. Chandra, Mallojjala Sharath Banerjee, Ankita Lahiri, Surobhi Pulipeta, Mallikarjuna CHAKRAPANI, HARINATH Rangarajan, Radha Dept. of Chemistry |
| Keywords: | Bioreductively Activated Oxygen Species MRSA Inhibitors Aureus infections Antibacterial activity 2014 |
| Issue Date: | Jul-2014 |
| Publisher: | American Chemical Society |
| Citation: | ACS Medicinal Chemistry Letters, 5(7), 777-781. |
| Abstract: | The number of cases of drug resistant Staphylococcus aureus infections is on the rise globally and new strategies to identify drug candidates with novel mechanisms of action are in urgent need. Here, we report the synthesis and evaluation of a series of benzo[b]phenanthridine-5,7,12(6H)-triones, which were designed based on redox-active natural products. We find that the in vitro inhibitory activity of 6-(prop-2-ynyl)benzo[b]phenanthridine-5,7,12(6H)-trione (1f) against methicillin-resistant Staphylococcus aureus (MRSA), including a panel of patient-derived strains, is comparable or better than vancomycin. We show that the lead compound generates reactive oxygen species (ROS) in the cell, contributing to its antibacterial activity. |
| URI: | http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/1926 https://doi.org/10.1021/ml5001118 |
| ISSN: | 1948-5875 1948-5875 |
| Appears in Collections: | JOURNAL ARTICLES |
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