2. Academic Validation
  3. Pyrroles and other heterocycles as inhibitors of p38 kinase

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

Affiliation

  • 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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