Literature DB >> 12127515

SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.

Laszlo Revesz1, Franco E Di Padova, Thomas Buhl, Roland Feifel, Hermann Gram, Peter Hiestand, Ute Manning, Romain Wolf, Alfred G Zimmerlin.   

Abstract

2,6-Diamino-3,5-difluoropyridinyl substituted pyridinylimidazoles, -pyrroles, -oxazoles, -thiazoles and -triazoles have been identified as novel p38alpha inhibitors. Pyridinylimidazole 11 potently inhibited LPS-induced TNFalpha in mice, showed good efficacy in the established rat adjuvant (ED(50): 10 mg/kg po b.i.d.) and collagen induced arthritis (ED(50): 5 mg/kg po b.i.d.) with disease modifying properties based on histological analysis of the joints.

Entities:  

Mesh:

Substances:

Year:  2002        PMID: 12127515     DOI: 10.1016/s0960-894x(02)00336-0

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


  4 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.  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

3.  Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Authors:  Joshua Almond-Thynne; David C Blakemore; David C Pryde; Alan C Spivey
Journal:  Chem Sci       Date:  2016-08-09       Impact factor: 9.825

4.  An Efficient One-Pot Catalyzed Synthesis of 2,4-Disubstituted 5-Nitroimidazoles Displaying Antiparasitic and Antibacterial Activities.

Authors:  Fanny Mathias; Youssef Kabri; Liliane Okdah; Carole Di Giorgio; Jean-Marc Rolain; Cédric Spitz; Maxime D Crozet; Patrice Vanelle
Journal:  Molecules       Date:  2017-08-03       Impact factor: 4.411

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.