51649-80-0Relevant articles and documents
Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
Dos Santos, Maurício Silva,Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo
, p. 335 - 343 (2021/09/07)
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.
Selective targeting of the αC and DFG-out pocket in p38 MAPK
R?hm, Sandra,Schr?der, Martin,Dwyer, Jessica E.,Widdowson, Caroline S.,Chaikuad, Apirat,Berger, Benedict-Tilman,Joerger, Andreas C.,Kr?mer, Andreas,Harbig, Jule,Dauch, Daniel,Kudolo, Mark,Laufer, Stefan,Bagley, Mark C.,Knapp, Stefan
, (2020/10/09)
The p38 MAPK cascade is a key signaling pathway linked to a multitude of physiological functions and of central importance in inflammatory and autoimmune diseases. Although studied extensively, little is known about how conformation-specific inhibitors alter signaling outcomes. Here, we have explored the highly dynamic back pocket of p38 MAPK with allosteric urea fragments. However, screening against known off-targets showed that these fragments maintained the selectivity issues of their parent compound BIRB-796, while combination with the hinge-binding motif of VPC-00628 greatly enhanced inhibitor selectivity. Further efforts focused therefore on the exploration of the αC-out pocket of p38 MAPK, yielding compound 137 as a highly selective type-II inhibitor. Even though 137 is structurally related to a recent p38 type-II chemical probe, SR-318, the data presented here provide valuable insights into back-pocket interactions that are not addressed in SR-318 and it provides an alternative chemical tool with good cellular activity targeting also the p38 back pocket.
Pyrazolo pyrimidine derivative and its preparation method and application (by machine translation)
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Paragraph 0042; 0043; 0044; 0047, (2019/10/23)
The invention discloses a pyrazolo pyrimidine ketone derivatives, wherein R1 For nicotinic acid, isonicotinic acid, 2 - chloro nicotinic acid, 6 - chloro nicotinic acid, 2 - bromo nicotinic acid, 6 - bromo nicotinic acid, 2 - fluoro nicotinic acid, 6 - fluoro nicotinic acid, 6 - methoxy nicotinic acid or 2 - methoxy nicotinic acid; R2 Hydrogen, fluoro, chloro or methyl; R3 Is hydrogen or methyl. Also disclosed the preparation method of the derivative and application, by chemical synthetic way to synthesize 40 for the purpose of the compound, and further by the introduction of the the purpose of the chiral compound to the secondary structure is optimized, so that the preparation of the pyrazole and pyrimidinone derivatives with broad-spectrum of cooperativity antifungal activity, in particular to the apple rot bacteria and germ inhibiting activity represent significant; the application in order to develop pyrazolo pyrimidine compound derivatives as the active ingredient to provide the basis for a novel bactericide. (by machine translation)