4343-75-3Relevant articles and documents
Fragment-Based Discovery of Dual JC Virus and BK Virus Helicase Inhibitors
Bonafoux, Dominique,Nanthakumar, Suganthini,Bandarage, Upul K.,Memmott, Christine,Lowe, Derek,Aronov, Alex M.,Bhisetti, Govinda Rao,Bonanno, Kenneth C.,Coll, Joyce,Leeman, Joshua,Lepre, Christopher A.,Lu, Fan,Perola, Emanuele,Rijnbrand, Rene,Taylor, William P.,Wilson, Dean,Zhou, Yi,Zwahlen, Jacque,Ter Haar, Ernst
, p. 7138 - 7151 (2016)
There are currently no treatments for life-threatening infections caused by human polyomaviruses JCV and BKV. We therefore report herein the first crystal structure of the hexameric helicase of JCV large T antigen (apo) and its use to drive the structure-based design of dual JCV and BKV ATP-competitive inhibitors. The crystal structures obtained by soaking our early inhibitors into the JCV helicase allowed us to rapidly improve the biochemical activity of our inhibitors from 18 μM for the early 6-(2-methoxyphenyl)- and the 6-(2-ethoxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole hits 1a and 1b to 0.6 μM for triazolopyridine 12i. In addition, we were able to demonstrate measurable antiviral activity in Vero cells for our thiazolopyridine series in the absence of marked cytotoxicity, thus confirming the usefulness of this approach.
HERBICIDAL COMPOUNDS
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Page/Page column 74, (2021/04/10)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
HCK INHIBITORS FOR THE TREATMENT OF FIBROSIS AND CANCER
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Paragraph 00104, (2020/10/20)
Compounds which are thiazole and triazole derivatives are disclosed, including compounds of the following genus: Formula I. The compounds are inhibitors of hematopoietic cell kinase (HCK) and exhibit anti-fibrotic and anti-proliferative effects. They are useful in the treatment of a variety of disorders, including a fibrosis or a fibrotic disease, such as renal fibrosis.
Synthesis, characterization, and biological activity of some novel Schiff bases and their Co(II) and Ni(II) complexes: A new route for Co3O4 and NiO nanoparticles for photocatalytic degradation of methylene blue dye
Nassar, Mostafa Y.,Aly, Hisham M.,Abdelrahman, Ehab A.,Moustafa, Moustafa E.
, p. 462 - 471 (2017/05/09)
Six novel Co(II) and Ni(II)-triazole Schiff base complexes have been successfully synthesized by refluxing the prepared triazole Schiff bases with CoCl2·6H2O or NiCl2·6H2O. The Schiff base ligands were prepared through condensation of 3-R-4-amino-5-hydrazino-1,2,4-triazole with dibenzoylmethane [R[dbnd]H, CH3, and CH2CH3; namely, L1, L2, and L3, respectively]. The prepared Co(II) and Ni(II) complexes have been identified using elemental analysis, FT-IR, UV–Vis, magnetic moment, conductivity, and thermal analysis. On the basis of the conductance results, it was concluded that all the prepared complexes are nonelectrolytes. Interestingly, the prepared Co(II) and Ni(II) complexes were employed as precursors for producing of Co3O4 and NiO nanoparticles, respectively. The produced nanostructures have been identified by XRD, HR-TEM, FT-IR and UV–Vis spectra. The produced nanoparticles revealed good photocatalytic activity for the degradation of methylene blue dye under UV illumination in presence of hydrogen peroxide. The percent of degradation was estimated to be 55.71% in 420.0?min and 90.43% in 360.0?min for Co3O4 and NiO, respectively. Moreover, the synthesized complexes, nano-sized Co3O4, and NiO products have been examined, employing modified Bauer- Kirby method, for antifungal (Candida albicans and Aspergillus flavus) and antibacterial (Staphylococcus aureus and Escherichia coli) activities.