185557-07-7Relevant academic research and scientific papers
Dihydropyrrolones as bacterial quorum sensing inhibitors
Almohaywi, Basmah,Yu, Tsz Tin,Iskander, George,Chan, Daniel S.H.,Ho, Kitty K.K.,Rice, Scott,Black, David StC.,Griffith, Renate,Kumar, Naresh
supporting information, p. 1054 - 1059 (2019/03/13)
Bacteria regulate their pathogenicity and biofilm formation through quorum sensing (QS), which is an intercellular communication system mediated by the binding of signaling molecules to QS receptors such as LasR. In this study, a range of dihydropyrrolone (DHP) analogues were synthesized via the lactone-lactam conversion of lactone intermediates. The synthesized compounds were tested for their ability to inhibit QS, biofilm formation and bacterial growth of Pseudomonas aeruginosa. The compounds were also docked into a LasR crystal structure to rationalize the observed structure-activity relationships. The most active compound identified in this study was compound 9i, which showed 63.1% QS inhibition of at 31.25 μM and 60% biofilm reduction at 250 μM with only moderate toxicity towards bacterial cell growth.
Pyridazine N-oxides. I. Synthesis and in vitro antimicrobial evaluation of 3-methyl-4-aryl-6-R-pyridazine N-oxides
Gavini,Juliano,Mule,Pirisino,Pinna,Curzu
, p. 683 - 688 (2007/10/03)
A new series of 3-methyl-4-aryl-6-R-pyridazine N-oxides 1a-j, structurally related to known antifungal agents azoxybacillin and pyridazomycin, has been prepared and evaluated for their in vitro antimicrobial activity. Among the compounds synthesized only 1g and 1h showed a fair activity against Gram-positive Staphylococcus epidermidis and Staphylococcus aureus.
