Literature DB >> 20570148

The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.

Kenneth Down1, Paul Bamborough, Catherine Alder, Amanda Campbell, John A Christopher, Maria Gerelle, Steve Ludbrook, Dave Mallett, Geoff Mellor, David D Miller, Rosannah Pearson, Keith Ray, Yemisi Solanke, Don Somers.   

Abstract

A novel pyrrole-2-carboxamide series of p38alpha inhibitors, discovered through the application of virtual screening, is presented. Following evaluation of activity, selectivity and developability properties of commercially available analogues, a synthesis program enabled rapid assessment of the series' suitability for further lead optimisation studies. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20570148     DOI: 10.1016/j.bmcl.2010.05.011

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


  2 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

Review 2.  Recent approaches in the organocatalytic synthesis of pyrroles.

Authors:  Biplob Borah; Kartikey Dhar Dwivedi; L Raju Chowhan
Journal:  RSC Adv       Date:  2021-04-13       Impact factor: 3.361

  2 in total

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