The quorum sensing (QS) system in multi-drug-resistant bacteria such as is primarily responsible for the development of antibiotic resistance and is considered an attractive target for antimicrobial drug discovery. In this study, we synthesised a series of novel selenourea and thiourea-containing dihydropyrrol-2-one (DHP) analogues as LasR antagonists. The selenium DHP derivatives displayed significantly better quorum-sensing inhibition (QSI) activities than the corresponding sulphur analogues. The most potent analogue efficiently inhibited the QS system by 81% at 125 µM and 53% at 31 µM. Additionally, all the compounds were screened for their minimum inhibitory concentration (MIC) against the Gram-positive bacterium , and interestingly, only the selenium analogues showed antibacterial activity, with and being the most potent with a MIC of 15.6 µM.
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| http://dx.doi.org/10.3390/antibiotics10030321 | DOI Listing |
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