Novel Seleno- and Thio-Urea Containing Dihydropyrrol-2-One Analogues as Antibacterial Agents
The quorum sensing (QS) system in multi-drug-resistant bacteria such as <i>P. aeruginosa</i> 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 sele...
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| Main Authors: | , , , , , , , , |
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| Format: | Book |
| Published: |
MDPI AG,
2021-03-01T00:00:00Z.
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| Summary: | The quorum sensing (QS) system in multi-drug-resistant bacteria such as <i>P. aeruginosa</i> 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 <b>3e</b> efficiently inhibited the <i>las</i> 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 <i>S. aureus</i>, and interestingly, only the selenium analogues showed antibacterial activity, with <b>3c</b> and <b>3e</b> being the most potent with a MIC of 15.6 µM. |
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| Item Description: | 10.3390/antibiotics10030321 2079-6382 |