Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370395 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
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 p38α 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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Paul Eastwood, Jacob González, Elena Gómez, Francisco Caturla, Nuria Aguilar, Marta Mir, Josep Aiguadé, Victor Matassa, Cristina Balagué, Adelina Orellana, María Domínguez,