1060811-62-2Relevant articles and documents
A Facile Synthesis of New 4,6-Dichloropyridine Derivatives, Their Biological Evaluation for Antimicrobial and Antioxidant Activity, and Docking Studies
Singaram, Kulathooran,Marimuthu, Dhamodaran,Baskaran, Selvakumar,Chinaga, Sureshkumar
, p. 758 - 769 (2016)
A facile synthesis of new 4,6-dichloropyridine derivatives 5(a–f), 6(a–c), and 7(a–c) were synthesized using both conventional heating and solvent-free microwave irradiation techniques. The results revealed that the latter method is superior to the conventional heating method. The easy work-up of the products, rapid reaction, and mild conditions are noticeable features of this protocol. Structural elucidation of the synthesized compounds was made on the basis of various spectroscopic methods. The synthesized compounds were evaluated for their in vitro antimicrobial activity (minimum inhibitory concentration; MIC) against various microbial strains using the agar well-diffusion method. Among the compounds, 5c showed best antimicrobial activity against most of the employed strains, especially against Staphylococcus aureus, Escherichia coli, Rhizopus arrhizus, and Candida albicans. Compounds 5a, 6a, 6c, 7a, and 7c showed significant antioxidant activity when compared to the other compounds. In addition to this, theoretical docking studies were performed for the highly potent compounds 5a, 6a, 6c, 7a, and 7c against three different drug targets belonging to the oxidoreductase family, and the results were found to be highly satisfactory.
TRICYCLIC KINASE INHIBITORS AND USE THEREOF
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, (2021/03/13)
The present application provides novel compounds that are inhibitors of kinases, including AMPK-related kinases like NUAK1, NUAK2, SIK1, SIK2, SIK3, MARK1, MARK2, MARK3, MARK4, as well as AURKA, AURKB, AURKC, CLK1, CLK2, DCAMKL2, MAPK7, MKNK2, PIK3CD, PKN3, RET, TAOK1, TAOK2, TAOK3, ULK2 and their mutants. The application also provides compositions, including pharmaceutical compositions, kits that include compounds, and methods of making and using compounds. The compounds provided herein are useful in treating diseases, disorders, or conditions that are mediated by these kinases.
CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR PREPARING THE SAME
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Page/Page column 66; 68, (2018/12/13)
The present disclosure relates to solid forms of N-{[2'-(2,6-difluoro-3,5-dimethoxyphenyl)-3'-oxo-2',3'-dihydro-1'H-spiro[cyclopropane-1,4'-[2,7]naphthyridin]-6'-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.