Browsing by Author Truong, Thanh Tung
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The threats of drug resistance and new emerging pathogens have led to an urgent need to develop alternative treatment therapies. Recently, considerable research efforts have focused on membrane-active peptides (MAPs), a category of peptides in drug discovery with antimicrobial, anticancer, and cell penetration activities that have demonstrated their potential to be multifunctional agents. Nonetheless, natural MAPs have encountered various disadvantages, which mainly include poor bioavailability, the lack of a secondary structure in short peptides, and high production costs for long peptide sequences. Hence, an “all-hydrocarbon stapling system” has been applied to these peptides and pr... |
Herein, a library of novel hybrid 6-(4-substituted-1H-1,2,3-triazol-1-yl)-2-mercaptobenzothiazoles was designed using a “left-hand strategy” and synthesized using microwave-assisted synthesis. The synthesized compounds were screened against quorum sensing activities and biofilm formation of Gram-negative bacteria. Biological results reveal that eleven compounds strongly inhibited the quorum sensing activities of the Pseudomonas aeruginosa lasB-gfp reporter strain.Compounds 4g (IC50 of 9.84 ± 1.10 μM), 4h (IC50 of 6.09 ± 0.98 μM), and 4m (IC50 of 12.20 ± 0.25 μM) are 2–5 times stronger than the reference compound 4NPO (IC50 of 32 ± 0.88 μM) in QSI screening. Compounds 4g and 4h inh... |
