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Structure-based design of benzofuran library as P. aeruginosa Quorum sensing inhibitors: Synthesis, biological evaluation and Molecular docking study.

Research Abstract

Two series of benzofuran-based thiosemicarbazides 7, 8(a-l) are evaluated as P. aeruginosa quorum sensing inhibitors (QSIs). The studied compounds resulted in reduction of violacein production of C. violaceum, at ¼ MIC, up to 26.04 – 67.36%, relative to the reference drug azithromycin (54%). In vitro evaluation of QS and antivirulence activities, at the same concentration, against P. aeruginosa, showed promising inhibitory effect of biofilms formation, bacterial motility and virulence factors production (pyocyanin, and rhamnolipids). Compounds 7a, 7d, and 7k inhibit biofilm formation up to 57.31%, 67.54%, 78.38%, respectively, in addition to > 50% inhibition of hemolysin production. On the other hand, compounds 8a, 8d, 8f and 8k of the bromobenzofuran series showed, 55.66%, 50.67%, 73.34%, 79.93%, reduction in biofilm formation, respectively. Compounds 8d and 8f exhibit > 50% reduction of hemolysin

Research Authors
Shaimaa I. Nazeih Noha G. Mohamed, Wesam S. Qayed, Mahmoud M. Sheha, Farghaly A. Omar, Wael AH. Hegazy
Research Date
Research Journal
European Journal of Medicinal Chemistry
Research Year
2025