91093-69-5Relevant academic research and scientific papers
Design, synthesis and evaluation of thiazole based amides for their antitubercular and PknG inhibitory activity
Sharma, Anindra
, p. 624 - 632 (2021/09/28)
A series of thiazole based amides have been designed and synthesized by solution-phase amide coupling of 2-aminothiazole and its derivatives with naturally occurring aromatic and heteroaromatic acids in excellent yield via DIC/HOBt protocol All the compounds have been evaluated for their antitubercular activity against M. tuberculosis virulent strain M. tuberculosis H37Rv and PknG inhibitory activity in the presence and absence of the inhibitors The compounds display moderate to significant PknG inhibitory activity (9.1-15.6% inhibition at 100 μM) as compared to the standard inhibitors and very moderate in vitro antitubercular activities against M. tuberculosis virulent strain M. tuberculosis H37Rv.
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.
