42044-81-5Relevant academic research and scientific papers
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.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 69, (2010/11/18)
This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure
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)).
Tobacco smoke chemistry. 2. Alkyl and alkenyl substituted guaiacols found in cigarette smoke condensate.
Arnarp,Bielawski,Dahlin,Dahlman,Enzell,Pettersson
, p. 44 - 50 (2007/10/02)
A series of alkyl and alkenyl substituted guaiacols, which comprise a group of biologically and organoleptically active compounds, have been synthesized. Mass spectra and GC retention times for these have been recorded and compared with those obtained for constituents of a weakly acidic fraction of smoke condensate derived from American blend type cigarettes. On the basis of these results, 25 guaiacols have been identified, 18 of which have not been detected in tobacco smoke condensate previously.
