Literature DB >> 18325768

The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.

Antonio Garrido Montalban1, Erik Boman, Chau-Dung Chang, Susana Conde Ceide, Russell Dahl, David Dalesandro, Nancy G J Delaet, Eric Erb, Justin T Ernst, Andrew Gibbs, Jeffrey Kahl, Linda Kessler, Jan Lundström, Stephen Miller, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Robert Sullivan, Zhijun Wang, Christopher J Larson.   

Abstract

We have identified a novel series of potent p38 MAP kinase inhibitors through structure-based design which due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME and in vivo PK studies show these compounds to have drug-like characteristics which could result in the development of an oral treatment for inflammatory conditions.

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Year:  2008        PMID: 18325768     DOI: 10.1016/j.bmcl.2008.02.033

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Microwave irradiation: synthesis and characterization of α-ketoamide and bis (α-ketoamide) derivatives via the ring opening of N-acetylisatin.

Authors:  Ayman El-Faham; Sherine N Khattab; Hazem A Ghabbour; Hoong-Kun Fun; M Rafiq H Siddiqui
Journal:  Chem Cent J       Date:  2014-04-28       Impact factor: 4.215

  1 in total

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