6292-58-6Relevant articles and documents
Preparation method and medical application of benzisothiazole and benzothiophene
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Paragraph 0166-0169; 0190-0192, (2021/08/19)
The invention discloses a preparation method and medical application of benzisothiazole and benzothiophene, and telates to the field of pharmaceutical chemistry. According to the invention, benzisothiazole and benzothiophene are the first type of HIF-2 agonists; compared with a compound M1001 found by the applicant in the earlier stage, the invention has better HIF-2 agonist activity, and has remarkable enhancement activity on expression of mRNA and protein of EPO, VGEF, Glut1, NDRG1 and the like at the downstream of HIF-2, so that the invention can be used for preparing drugs for treating and/or preventing chronic kidney diseases/chronic renal anemia, dyslipidemia and high cholesterol caused by abnormal expression of HIF-2; and the method has a good industrialization prospect.
Multiprotein Dynamic Combinatorial Chemistry: A Strategy for the Simultaneous Discovery of Subfamily-Selective Inhibitors for Nucleic Acid Demethylases FTO and ALKBH3
Das, Mohua,Yang, Tianming,Dong, Jinghua,Prasetya, Fransisca,Xie, Yiming,Wong, Kendra H. Q.,Cheong, Adeline,Woon, Esther C. Y.
supporting information, p. 2854 - 2867 (2018/09/25)
Dynamic combinatorial chemistry (DCC) is a powerful supramolecular approach for discovering ligands for biomolecules. To date, most, if not all, biologically templated DCC systems employ only a single biomolecule to direct the self-assembly process. To expand the scope of DCC, herein, a novel multiprotein DCC strategy has been developed that combines the discriminatory power of a zwitterionic “thermal tag” with the sensitivity of differential scanning fluorimetry. This strategy is highly sensitive and could differentiate the binding of ligands to structurally similar subfamily members. Through this strategy, it was possible to simultaneously identify subfamily-selective probes against two clinically important epigenetic enzymes: FTO (7; IC50=2.6 μm) and ALKBH3 (8; IC50=3.7 μm). To date, this is the first report of a subfamily-selective ALKBH3 inhibitor. The developed strategy could, in principle, be adapted to a broad range of proteins; thus it is of broad scientific interest.
PROCESS FOR PREPARING 1,1,3-TRIOXO-1,2-BENZOTHIAZOLE-6-CARBOXAMIDE
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Page/Page column 21, (2017/07/31)
A process for preparing, 1,1,3-trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: (a) oxidizing 2,5-dimethyl-benzenesulfonamide of formula (II) in the presence of an oxidizing agent to receive 2-sulfamoyl-terephthalic acid of formula (III);
Oxidatively sonochemical dealkylation of various N-alkylsulfonamides to free sulfonamides and aldehydes
Katohgi, Masashi,Togo, Hideo
, p. 7481 - 7486 (2007/10/03)
Various N-alkylsulfonamides were easily dealkylated to give the corresponding free sulfonamides in moderate to good yields in the presence of (diacetoxyiodo)benzene and iodine under ultrasonic irradiation. Application of this methodology to various N-prot
Novel sonochemical dealkylation of N-alkylsulfonamides in the presence of (diacetoxyiodo)benzene and iodine
Katohgi, Masashi,Yokoyama, Masataka,Togo, Hideo
, p. 1055 - 1057 (2007/10/03)
Various N-alkylsulfonamides were easily dealkylated in moderate to good yields by the ultrasonic irradiation in the presence of (diacetoxyiodo)benzene and iodine.