Literature DB >> 15837335

Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase.

Nuria Tamayo1, Lillian Liao, Martin Goldberg, David Powers, Yan-Yan Tudor, Violeta Yu, Lu Min Wong, Bradley Henkle, Scot Middleton, Rashid Syed, Timothy Harvey, Graham Jang, Randall Hungate, Celia Dominguez.   

Abstract

Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-alpha production in mice and exhibited good efficacy in the rat collagen induced arthritis model.

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Year:  2005        PMID： 15837335     DOI： 10.1016/j.bmcl.2005.02.010

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


  3 in total

1.  Virtual screening using a conformationally flexible target protein: models for ligand binding to p38α MAPK.

Authors:  Natalie B Vinh; Jamie S Simpson; Peter J Scammells; David K Chalmers
Journal:  J Comput Aided Mol Des       Date:  2012-04-20       Impact factor: 3.686

2.  An Evaluation of Explicit Receptor Flexibility in Molecular Docking Using Molecular Dynamics and Torsion Angle Molecular Dynamics.

Authors:  Roger S Armen; Jianhan Chen; Charles L Brooks
Journal:  J Chem Theory Comput       Date:  2009-10-13       Impact factor: 6.006

3.  A convenient one-pot synthesis of 3-amino-2, 5-dihydropyridazine and pyrimidine derivatives in the presence of high surface area MgO as a highly effective heterogeneous base catalyst.

Authors:  Hassan Sheibani; Mohammad Ali Amrollahi; Zeinab Esfandiarpoor
Journal:  Mol Divers       Date:  2009-06-19       Impact factor: 2.943
  3 in total

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