Literature DB >> 9873604

Pyrroles and other heterocycles as inhibitors of p38 kinase.

S E de Laszlo1, D Visco, L Agarwal, L Chang, J Chin, G Croft, A Forsyth, D Fletcher, B Frantz, C Hacker, W Hanlon, C Harper, M Kostura, B Li, S Luell, M MacCoss, N Mantlo, E A O'Neill, C Orevillo, M Pang, J Parsons, A Rolando, Y Sahly, K Sidler, S J O'Keefe.   

Abstract

Investigation of furans, pyrroles and pyrazolones identified 3-pyridyl-2,5-diaryl-pyrroles as potent, orally bioavailable inhibitors of p38 kinase. 3-(4-pyridyl-2-(4-fluoro-phenyl)-5-(4-methylsulfinylphenyl)-pyrrol e (L-167307) reduces secondary paw swelling in the rat adjuvant arthritis model: ID50 = 7.4 mg/kg/b.i.d.

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Year:  1998        PMID： 9873604     DOI： 10.1016/s0960-894x(98)00495-8

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


  12 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.  Development of an online p38α mitogen-activated protein kinase binding assay and integration of LC-HR-MS.

Authors:  David Falck; Jon S B de Vlieger; Wilfried M A Niessen; Jeroen Kool; Maarten Honing; Martin Giera; Hubertus Irth
Journal:  Anal Bioanal Chem       Date:  2010-08-22       Impact factor: 4.142

3.  Slack sodium-activated potassium channel membrane expression requires p38 mitogen-activated protein kinase phosphorylation.

Authors:  Sushmitha Gururaj; John Fleites; Arin Bhattacharjee
Journal:  Neuropharmacology       Date:  2015-12-22       Impact factor: 5.250

4.  Rough lipopolysaccharide from Brucella abortus and Escherichia coli differentially activates the same mitogen-activated protein kinase signaling pathways for tumor necrosis factor alpha in RAW 264.7 macrophage-like cells.

Authors:  Bruce W Jarvis; Tajie H Harris; Nilofer Qureshi; Gary A Splitter
Journal:  Infect Immun       Date:  2002-12       Impact factor: 3.441

5.  Construction of 4D-QSAR models for use in the design of novel p38-MAPK inhibitors.

Authors:  Nelilma Correia Romeiro; Magaly Girão Albuquerque; Ricardo Bicca de Alencastro; Malini Ravi; Anton J Hopfinger
Journal:  J Comput Aided Mol Des       Date:  2005-06       Impact factor: 3.686

6.  SD0006: a potent, selective and orally available inhibitor of p38 kinase.

Authors:  Barry L Burnette; Shaun Selness; Raj Devraj; Gail Jungbluth; Ravi Kurumbail; Loreen Stillwell; Gary Anderson; Stephen Mnich; Jeffrey Hirsch; Robert Compton; Pamela De Ciechi; Heidi Hope; Michael Hepperle; Robert H Keith; Win Naing; Huey Shieh; Joseph Portanova; Yan Zhang; Jian Zhang; Richard M Leimgruber; Joseph Monahan
Journal:  Pharmacology       Date:  2009-07-04       Impact factor: 2.547

7.  4-(4-Fluoro-phen-yl)-2-methyl-3-(1-oxy-4-pyridyl)isoxazol-5(2H)-one.

Authors:  Simona Margutti; Dieter Schollmeyer; Stefan Laufer
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-01-23

8.  Leptin regulates tau phosphorylation and amyloid through AMPK in neuronal cells.

Authors:  Steven J Greco; Sraboni Sarkar; Jane M Johnston; Nikolaos Tezapsidis
Journal:  Biochem Biophys Res Commun       Date:  2009-01-21       Impact factor: 3.575

9.  4-[4-(4-Fluoro-phen-yl)-2-methyl-5-oxo-2,5-dihydro-isoxazol-3-yl]-1-methyl-pyridinium iodide-4-[3-(4-fluoro-phen-yl)-2-methyl-5-oxo-2,5-dihydro-isoxazol-4-yl]-1-methyl-pyridinium iodide (0.6/0.4).

Authors:  Simona Margutti; Dieter Schollmeyer; Stefan Laufer
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2007-12-18

10.  4-[2-(4-Fluoro-phen-yl)-1H-pyrrol-3-yl]pyridine.

Authors:  Bassam Abu Thaher; Pierre Koch; Dieter Schollmeyer; Stefan Laufer
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-02-04
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