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Bioorg Med Chem Lett. 2011 Nov 1;21(21):6253-7. doi: 10.1016/j.bmcl.2011.09.006. Epub 2011 Sep 10.

Indolin-2-one p38α inhibitors III: bioisosteric amide replacement.

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1
Almirall Research Center, Almirall Laboratories, Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain. paul.eastwood@almirall.com

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.

PMID:
21958544
DOI:
10.1016/j.bmcl.2011.09.006
[Indexed for MEDLINE]
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