20951-00-2Relevant articles and documents
Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects
Han, Yufei,Huang, Desheng,Xu, Sicong,Li, Lingling,Tian, Ye,Li, Shuo,Chen, Cong,Li, Yingxiu,Sun, Yanping,Hou, Yunlei,Sun, Yongjun,Qin, Mingze,Gong, Ping,Gao, Zibin,Zhao, Yanfang
, (2020/12/07)
Inhibition of the soluble epoxide hydrolase (sEH) is a promising new therapeutic approach in the treatment of inflammation. Driven by the in-house database product lead 1, a hybridization strategy was utilized for the design of a series of novel benzo [d]thiazol derivatives. To our delight, D016, a byproduct of compound 9, was obtained with an extraordinarily low IC50 value of 0.1 nM but poor physical and chemical properties. After removal of a non-essential urea moiety or replacement of the urea group by an amide group, compounds 15a, 17p, and 18d were identified as promising sEH inhibitors, and their molecular binding modes to sEH were constructed. Furthermore, compounds 15a and 18d exhibited more effective in vivo anti-inflammatory effect than t-AUCB in carrageenan-induced mouse paw edema. Compound 15a also showed moderate metabolic stability with a half-time of 34.7 min. Although 18d was unstable in rat liver microsomes, it might be a “prodrug”. In conclusion, this study could provide valuable insights into discovery of new sEH inhibitors, and compounds 15a and 18d were worthy of further development as potential drug candidates to treat inflammation.
Benzothiazole derivatives and their uses
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Paragraph 0163; 0165; 0166; 0181; 0182, (2022/01/05)
The present invention relates to benzothiazole derivatives and their uses, specifically to compounds shown in formula I or stereoisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, methods of preparation thereof, and pharmaceutical compositions containing the compounds, wherein the substituentsR1,R2,R8 , X, Y, Z, Q have the meaning given in the instruction manual. The present invention further relates to the application of compounds of formula I in the preparation of drugs for the treatment and / or prevention of sEH-mediated diseases, in particular in the preparation of drugs for the treatment of inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes mellitus, diabetic complications, diabetes-related diseases, fibrotic diseases, neurological and psychiatric diseases, pain, ulcerative diseases and the like.
BENZOTHIADIAZINE DERIVATIVES AND COMPOSITIONS COMPRISING THE SAME FOR TREATING DISORDERS MEDIATED BY ADENOSINE
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Page/Page column 30; 32; 55, (2020/07/15)
Disclosed herein are novel inhibitors of CD73. More specifically, the novel CD73 inhibitors are derived from benzothiadiazine. Further, the present disclosure is related to the use of said benzothiadiazine derivatives in the treatment of diseases and/or d