50772-59-3Relevant articles and documents
Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds
Papadopoulou, Maria V.,Bloomer, William D.,Rosenzweig, Howard S.,Wilkinson, Shane R.,Szular, Joanna,Kaiser, Marcel
, p. 179 - 186 (2016)
A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as antitrypanosomatid agents. All tested compounds were active or moderately active against T
An extensive research on aldose reductase inhibitory effects of new 4H-1,2,4-triazole derivatives
Sever, Belgin,Alt?ntop, Mehlika Dilek,Demir, Yeliz,Pekdo?an, Muhammed,Akal?n ?ift?i, Gül?en,Beydemir, ?ükrü,?zdemir, Ahmet
, (2020/10/27)
Aldose reductase (AR) is a key enzyme, which triggers the excessive accumulation of sorbitol in insulin independent tissues leading to severe diabetes-induced microvascular complications. Substantial evidence has proven that AR inhibition is a well-establ
Design, synthesis, and biological evaluation of novel 1,3,4-thiadiazole derivatives as potential antitumor agents against chronic myelogenous leukemia: Striking effect of nitrothiazole moiety
Alt?ntop, Mehlika Dilek,Ciftci, Halil Ibrahim,Radwan, Mohamed O.,Sever, Belgin,Kaplanc?kl?, Zafer As?m,Ali, Taha F. S.,Koga, Ryoko,Fujita, Mikako,Otsuka, Masami,Zdemir, Ahmet
, (2018/01/05)
In an attempt to develop potent antitumor agents, new 1,3,4-thiadiazole derivatives were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the K562 chronic myelogenous leukemia cell line that expresses the Bcr-Abl tyrosine kinase. N-(5-Nitrothiazol-2-yl)-2-((5-((4-(trifluoromethyl)phenyl)amino)-1,3,4-thiadiazol-2-yl)thio)acetamide (2) inhibited the Abl protein kinase with an IC50 value of 7.4 μM and showed selective activity against the Bcr-Abl positive K562 cell line. Furthermore, a Bcr-Abl-compound 2 molecular modelling simulation highlighted the anchoring role of the nitrothiazole moiety in bonding and hydrophobic interaction with the key amino acid residues. These results provide promising starting points for further development of novel kinase inhibitors.
ANTIBACTERIAL THERAPEUTICS AND PROPHYLACTICS
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Paragraph 00307, (2017/02/24)
The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.