6558-36-7Relevant academic research and scientific papers
Targeting quorum sensing by designing azoline derivatives to inhibit the N-hexanoyl homoserine lactone-receptor CviR: Synthesis as well as biological and theoretical evaluations
Bucio-Cano, Alejandro,Reyes-Arellano, Alicia,Correa-Basurto, José,Bello, Martiniano,Torres-Jaramillo, Jenifer,Salgado-Zamora, Héctor,Curiel-Quesada, Everardo,Peralta-Cruz, Javier,Avila-Sorrosa, Alcives
, p. 7565 - 7577 (2015/12/18)
To counteract bacterial resistance, we investigated the interruption of quorum sensing mediated by non-classical bioisosteres of the N-hexanoyl homoserine lactone with an azoline core. For this purpose, a set of selected 2-substituted azolines was synthesized, establishing the basis for a new protocol to synthesize 2-amino imidazolines. The synthesized compounds were evaluated as inhibitors of violacein production in Chromobacterium violaceum. Theoretical studies on bioisostere-protein interactions were performed using CviR. The results show that some azolines decreased violacein production, suggesting an antiquorum sensing profile against Gram-negative bacteria. Docking and molecular dynamic simulations together with binding free energy calculations revealed the exact binding and inhibitory profiles. These theoretical results show relationship with the in vitro activity of the azoline series.
Ring-opened analogs of indomethacin affecting human neutrophil functions
Andreani, Aldo,Leoni, Alberto,Locatelli, Alessandra,Morigi, Rita,Rambaldi, Mirella,Gehret, Jean-Claude,Traniello, Serena,Cariani, Alessio,Spisani, Susanna
, p. 299 - 312 (2007/10/03)
A series of ring-opened analogs of indomethacin was synthesized and tested in vitro (at concentrations ranging from 10-9 to 10-5 mol/1) on human neutrophil functions. Two compounds lacking the carboxylic group were subjected to the s
Synthesis of 6,7-dihydrothiazolo[3,2-a]-1,3,5-triazine-4-aryl-2-thiones
Radha Rani,Rahman,Bhalerao
, p. 319 - 325 (2007/10/02)
Reaction of 2-aminothiazoline with aroylisothiocyanate gave 6,7-dihydrothiazolo[3,2-a]-1,3,5-triazine-4-aryl-2-thiones (5) in one step.
2-Aminothiazoline derivatives. Relationships between structure and antiinflammatory activity
Viallet,Boucherle,Cohen-Addad
, p. 553 - 559 (2007/10/05)
Pharmacological studies of 2-aminothiazoline amide and amine derivatives show these compounds to be actively anti-inflammatory. The structure determination by spectroscopic methods and X-ray diffraction indicates a relation between the structure and the activity of these compounds.
