| Literature DB >> 21958544 |
Paul Eastwood1, Jacob González, Elena Gómez, Francisco Caturla, Nuria Aguilar, Marta Mir, Josep Aiguadé, Victor Matassa, Cristina Balagué, Adelina Orellana, María Domínguez.
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.Entities:
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Year: 2011 PMID： 21958544 DOI： 10.1016/j.bmcl.2011.09.006
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823