Pyrroles and other heterocycles as inhibitors of p38 kinase

  • Bioorg Med Chem Lett. 1998 Oct 6;8(19):2689-94. doi: 10.1016/s0960-894x(98)00495-8.
S E de Laszlo  1 ,  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
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratory, Rahway, NJ 07065, USA.
PMID: 9873604 DOI: 10.1016/s0960-894x(98)00495-8
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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