42044-81-5Relevant articles and documents
cGAS ANTAGONIST COMPOUNDS
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Paragraph 0439, (2017/11/06)
Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
Hydroxyindole derivatives as inhibitors of IL-1 generation. II. Synthesis and pharmacological activities of (E)3-(7-hydroxy-6-methoxyindole-4-yl)-2-methylpropenoic acid derivatives
Tanaka,Okita,Akamatsu,Chiba,Obaishi,Nagakura,Sakurai,Yamatsu
, p. 187 - 198 (2007/10/03)
A series of (E)-3-(7-hydroxy-6-methoxyindole-4-yl)-2-methylpropenoic acid derivatives was prepared and the inhibitory activities of its members on IL-1 generation were evaluated in an in vitro system using exudate cells from the rat carboxy-methyl cellulose (CMC) induced air-pouch model. All the compounds in this new series were found to be inhibitors of IL-1 generation. In particular, the methoxy-substituted 2-phenyl compounds 28d-f were the most potent inhibitors of IL-1 generation (eg, 28d: IC50 = 0.8 μ,M). The compounds in this series also inhibited IL-1α and IL-1β generations in an in vitro system using human monocytes stimulated with LPS (eg, 28b: IC50 = 1.4 μM (IL-1α) and 0.9 μM (IL-1β)).