1192744-57-2Relevant academic research and scientific papers
Indolin-2-one p38α inhibitors III: Bioisosteric amide replacement
Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Aguilar, Nuria,Mir, Marta,Aiguadé, Josep,Matassa, Victor,Balagué, Cristina,Orellana, Adelina,Domínguez, María
, p. 6253 - 6257 (2011/11/29)
Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38a inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation.
New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
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Page/Page column 33, (2009/12/04)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
