Pyrroles and other heterocycles as inhibitors of P38 kinase
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)-pyrrole (L-167307) reduces secondary paw swelling in the rat adjuvant arthritis model: ID50 = 7.4 mg/kg/day.
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Cited by (119)
N-Heterocyclic Carbene-Catalyzed Condensation/ Oxidation/ Cyclization/ Aromatization Cascade for the Synthesis of Tri- and Tetra-Substituted Imidazoles
2023, Asian Journal of Organic ChemistryPaal–Knorr synthesis: An old reaction, new perspectives
2022, Advances in Heterocyclic ChemistryCitation Excerpt :This strategy nowadays, has been employed in synthesis of differently substituted pyrroles.33 3-Pyridyl-2,5-diaryl-pyrroles, found to be orally bioavailable inhibitors of p38 kinase, were synthesized via P–K reaction, exemplifying the prominence of this methodology.33 Similarly, several 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazoles derived from metronidazole were obtained and their antibacterial and antifungal potencies were positively examined.34
Conjugated pyrrole/aminoenone and pyrrole/aminoacrylonitrile ensembles: new motives in heterocyclic chemistry
2021, Mendeleev CommunicationsSlack sodium-activated potassium channel membrane expression requires p38 mitogen-activated protein kinase phosphorylation
2016, NeuropharmacologyCitation Excerpt :Anisomycin was purchased from Life Technologies. The p38 MAPK Inhibitor (C₂₀H₁₃ClFN₃O) was purchased from Millipore (de Laszlo et al. 1998). Since the cloning of the Slack channel in 1998, studies attempting to elucidate the structure of the channel have revealed that the KNa channels are set apart from the larger super-family of potassium channels by an extensive intracellular C-terminus (Joiner et al. 1998).
Anti-arthritic agents: Progress and potential
2015, Bioorganic and Medicinal ChemistryComparison of (bio-)transformation methods for the generation of metabolite-like compound libraries of p38α MAP kinase inhibitors using high-resolution screening
2014, Journal of Pharmaceutical and Biomedical Analysis
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