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2,4,5- triarylimidazole inhibitors of IL-1 biosynthesis
Abstract As part of an effort to define the pharmacophore and discover the mechanism by which the antiinflammatory dual cyclooxygenase / 5-lipoxygenase inhibitors SK&F 86002 and SK&F 105809 inhibitExpand
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.
Pyrimidine analogs of the pyrimidinylimidazole class of CSBP/p38 kinase inhibitors were prepared in an effort to reduce the potent inhibition of hepatic cytochrome P450 observed for the pyridinylExpand
1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency.
A series of 1-alkyl- or -aryl-4-aryl-5-pyridinylimidazoles (A) were prepared and tested for their ability to bind to a recently discovered protein kinase termed CSBP and to inhibit lipopolysaccharideExpand
Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea.
In vitro metabolic studies in mouse liver microsomes established enantiospecific glucuronidation as a likely mechanism for the observed differences between the enantiomers of 1a and (-)-1a. Expand
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
  • J. Adams, J. Boehm, +7 authors J. Lee
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 5 November 2001
Oral administration of inhibitors possessing a cyclohexan- 4-ol or piperidin-4-yl group at N-1 in combination with alkoxy, amino(alkyl), phenoxy and anilino substitution at the 2-position of the pyrimidine was found to potently inhibit LPS-induced TNF in mice and rats. Expand
Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.
Several nocathiacin I analogues (4-35) were synthesized and evaluated for their antibacterial activity and retained very good in vitro and in vivo antib bacterial activity. Expand
Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts.
The synthesis and antibacterial activity of a series of nocathiacin I derivatives (4-20) containing polar water solubilizing groups is described. Thiol-Michael adducts containing acidic polar groupsExpand
Novel semi-synthetic nocathiacin antibiotics: synthesis and antibacterial activity of bis- and mono-O-alkylated derivatives.
The excellent in vivo activity and improved water solubility of phosphate analogues 3m and 4g suggest their use as potential pro-drugs. Expand
Synthesis and antibacterial activity of nocathiacin I analogues.
Stereoselective reduction of dehydroalanine double bond in nocathiacin I afforded the primary amide 2, which upon coupling with a variety of amines furnished amides 4-32 that have retained very good antibacterial activity and improved aqueous solubility. Expand