19262-59-0Relevant academic research and scientific papers
Nitazoxanide analogues as antimicrobial agents against nosocomial pathogens
Gau, Jia-Suey,Lin, Wen-Pao,Kuo, Li-Ching,Hu, Ming-Kuan
, p. 544 - 552 (2016/09/04)
Background: The frequent use of antibacterial agents and the exposure of the patients to lifesaving intervention processes are consistently associated with the increased chance of nosocomial infections and the emergence of multidrug resistant microorganisms in the hospital environment. Thus, new antimicrobial agents are of unmet need to treat the severe nosocomial infections caused by these putative pathogens resistant to currently available agents. Method: Design, synthesis, and biological evaluation of analogues of nitazoxanide (NTZ), an FDA approved thiazolide antiparasitic, as new antimicrobial agents against nosocomial pathogens were described. The NTZ analogues were rationally explored on the basis of either increasing the electronic resonance effects at the nitrothiazolide moiety or improving the anionic form of the whole NTZ structure. Results: The MICs and MBCs values of these NTZ analogues against prevalent nosocomial pathogens were measured. The benzologous analogues 3a and 4a and p-chlorobenzenesulfonamides 8d and 9d exhibited tremendous antimicrobial activities, which were 100- To 2000-fold more potent than NTZ and ciprofloxacin. Conclusion: The results demonstrated that delicate manipulation of the NTZ core structure could lead to promising antimicrobial agents against the nosocomial pathogens.
Synthesis, in vitro and computational studies of protein tyrosine phosphatase 1B inhibition of a small library of 2-arylsulfonylaminobenzothiazoles with antihyperglycemic activity
Navarrete-Vazquez, Gabriel,Paoli, Paolo,Leon-Rivera, Ismael,Villalobos-Molina, Rafael,Medina-Franco, Jose Luis,Ortiz-Andrade, Rolffy,Estrada-Soto, Samuel,Camici, Guido,Diaz-Coutino, Daniel,Gallardo-Ortiz, Itzell,Martinez-Mayorga, Karina,Moreno-Diaz, Hermenegilda
experimental part, p. 3332 - 3341 (2009/09/08)
The 2-arylsulfonylaminobenzothiazole derivatives 1-27 were prepared using a one step reaction. The in vitro inhibitory activity of the compounds against protein tyrosine phosphatase 1B (PTP-1B) was evaluated. Compounds 4 and 16 are rapid reversible (mixed-type) inhibitors of PTP-1B with IC50 values in the low micromolar range. The most active compounds (4 and 16) were docked into the crystal structure of PTP-1B. Docking results indicate potential hydrogen bond interactions between the nitro group in both compounds and the catalytic amino acid residues Arg 221 and Ser 216. Both compounds were evaluated for their in vivo antihyperglycemic activity in a type 2 diabetes mellitus rat model, showing significant lowering of plasma glucose concentration, during the 7 h post-intragastric administration.
