1024448-92-7Relevant academic research and scientific papers
Synthesis and Antimicrobial Evaluation of Nitazoxanide-Based Analogues: Identification of Selective and Broad Spectrum Activity
Ballard, T. Eric,Wang, Xia,Olekhnovich, Igor,Koerner, Taylor,Seymour, Craig,Salamoun, Joseph,Warthan, Michelle,Hoffman, Paul S.,Macdonald, Timothy L.
experimental part, p. 362 - 377 (2012/01/11)
A library composed of nitazoxanide-based analogues was synthesized and assayed for increased antibacterial efficacy against the pyruvate-ferredoxin oxidoreductase (PFOR) using microorganisms Helicobacter pylori, Campylobacter jejuni and Clostridium difficile. Derivatives were found to recapitulate and improve activity against these organisms and select analogues were tested for their ability to disrupt the PFOR enzyme directly. The library was also screened for activity against staphylococci and resulted in the identification of analogues capable of inhibiting both staphylococci and all PFOR organisms at low micromolar minimum inhibitory concentrations with low toxicity to human foreskin cells. Hitting them where it hurts! A library of nitazoxanide-based analogues was synthesized and assayed for antibacterial efficacy against pyruvate-ferredoxin oxidoreductase (PFOR) utilizing microorganisms. Derivatives were found to recapitulate and improve activity against these organisms, and select analogues were screened for activity against staphylococci resulting in the identification of analogues capable of inhibiting both staphylococci and all PFOR organisms at low micromolar minimum inhibitory concentrations.
Discovery of new C3aR ligands. Part 1: Arginine derivatives
Denonne, Frederic,Binet, Sophie,Burton, Maggi,Collart, Philippe,Dipesa, Alan,Ganguly, Tanmoy,Giannaras, Alexander,Kumar, Seema,Lewis, Timothy,Maounis, Florence,Nicolas, Jean-Marie,Mansley, Tamsin,Pasau, Patrick,Preda, Dorin,Stebbins, Karin,Volosov, Alexander,Zou, Dong
, p. 3258 - 3261 (2008/02/08)
The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflamma
