82155-38-2Relevant academic research and scientific papers
Development of Chiral Ureates as Chiral Strong Br?nsted Base Catalysts
Ishikawa, Sho,Kondoh, Azusa,Terada, Masahiro
supporting information, p. 3724 - 3728 (2020/03/11)
Recently, chiral Br?nsted bases having high basicity have emerged as a powerful tool in developing new catalytic enantioselective reactions. However, such chiral strong Br?nsted base catalysts are still very scarce. Herein, we report the development of a chiral anionic Br?nsted base having a N,N′-dialkyl ureate moiety as a basic site. Its prominent catalytic activity was demonstrated in the enantioselective addition reactions of α-thioacetamides as less acidic pronucleophiles with various electrophiles. Thus, the newly developed chiral catalyst with high accessibility and structural tunability would expand the scope of viable enantioselective transformations under Br?nsted base catalysis.
Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors
Holmes, Christopher P.,Li, Xianfeng,Pan, Yijun,Xu, Caiding,Bhandari, Ashok,Moody, Claire M.,Miguel, Joy A.,Ferla, Steven W.,De Francisco, M. Nuria,Frederick, Brian T.,Zhou, Siqun,Macher, Natalie,Jang, Larry,Irvine, Jennifer D.,Grove, J. Russell
, p. 4336 - 4341 (2007/10/03)
A series of novel sulfonamides containing a single difluoromethylene- phosphonate group were discovered to be potent inhibitors of protein tyrosine phosphatase 1B. Structure-activity relationships around the scaffold were investigated, leading to the identification of compounds with IC50 or Ki values in the low nanomolar range. These sulfonamide-based inhibitors exhibit 100 and 30 times higher inhibitory activity than the corresponding tertiary amines and carboxamides, respectively.
Bicyclic pyrrolyl amides as glucogen phosphorylase inhibitors
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Page 57, (2010/02/06)
Heterocyclic amide derivatives, of formula (I): wherein —X-Y-Z- is selected from —S—CR4═CR5—, —CR4═CR5—S—, —O—CR4═CR5—, —CR4═CR5—O—, —N═CR4—S—, —S—CR4═N—, —NR6—CR4═CR5— and —CR4═CR5—NR6—; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof; (with provisos); possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
