- Microwave-assisted efficient synthesis of pyrazole-fibrate derivatives as stimulators of glucose uptake in skeletal muscle cells
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The design and synthesis of a series of pyrazolo[3,4-d]pyrimidinones containing fibrate side chains have been accomplished by utilizing the concept of molecular hybridization. All the synthesized compounds were evaluated for the glucose uptake stimulatory effect in L6 rat skeletal muscle cells. Four compounds (3f, 3g, 3j and 3q) were found to show significant stimulation of glucose uptake. Further these four compounds have been examined for their Glut4 translocation stimulatory effect in L6-Glut4myc myotubes. Compound 3q was found to exert maximum increase in GLUT4myc translocation.
- Gupta, Sampa,Kant, Ruchir,Pandey, Shubham,Rai, Amit Kumar,Sashidhara, Koneni V.,Singh, L. Ravithej,Tamrakar, Akhilesh K.
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- Piperidine compound and preparation method and medical application thereof
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The invention discloses a piperidine compound shown as a formula (I) and a preparation method and medical application thereof, and particularly relates to a piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof and a preparation method and application of the piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof. The compound provided by the invention can inhibit the activity of USP7 enzyme, has very good selectivity and druggability, and can be used for preparing medicines for preventing or treating tumor diseases or virus infectious diseases.
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Paragraph 0106-0108; 0110
(2021/04/07)
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- Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
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Hybrid systems containing pyrazole moiety show a wide spectrum of biological activities. To access novel hybrids with pyrazole ring, in this work we synthesized twenty pyrazole-carboxylic acids and twenty pyrazole-carboxamides, using simple synthetic methods, to be used as building blocks in the development of new structures.
- Dos Santos, Maurício Silva,Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo
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p. 335 - 343
(2021/09/07)
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- N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure–activity relationships and X-ray crystallographic studies
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USP7 as a deubiquitinase plays important roles in regulating the stability of some oncoproteins including MDM2 and DNMT1, and thus represents a potential anticancer target. Through comparative analysis of USP7 co-crystal structures in complex with the rep
- Chen, Caiping,Chen, Hui,Cheng, Keguang,Li, Minglei,Liu, Jun,Liu, Shengjie,Sun, Hongbin,Wang, Yue,Wen, Xiaoan,Xu, Qing-Long,Yuan, Haoliang,Zhou, Jin,Zhou, Shuxi,Zhou, Xinyu
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supporting information
(2020/06/03)
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- PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS
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The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5′ and R6 are described herein.
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Paragraph 2046; 2048
(2016/08/03)
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- 1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS FOR THE TEATMENT OF CNS DISORDERS
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The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterised by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X in
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Page/Page column 70; 72
(2009/07/03)
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- Microwave-assisted protocols for the expedited synthesis of pyrazolo[1,5-a] and [3,4-d]pyrimidines
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General, high-yielding MAOS protocols for the expedited synthesis of functionalized pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyrimidines, as well as their pyrazole precursors, are described amenable to an iterative analogue library synthesis strategy for lead optimization.
- Daniels, R. Nathan,Kim, Kwangho,Lebois, Evan P.,Muchalski, Hubert,Hughes, Mary,Lindsley, Craig W.
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p. 305 - 310
(2008/09/17)
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