期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 47, 期 11, 页码 2724-2727出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm049968m
关键词
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2-Aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-alpha) inhibitors, which contain a novel bicyclic pyrazolope core, are described. Many showed low-nanomolar activity against lipopolysaccharide-induced TNF-alpha production in monocytic cells. Secondary screening data are presented for the pyrimidinyl bicyclic pyrazolones. Several of these analogues showed good oral bioavailability in rat and efficacy in the rat iodoacetate in vivo model.
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