86930-90-7Relevant academic research and scientific papers
CHLORO-PYRAZINE CARBOXAMIDE DERIVATIVES WITH EPITHELIAL SODIUM CHANNEL BLOCKING ACTIVITY
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Paragraph 0481; 0482, (2014/06/25)
This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.
ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme
Gribble, Andrew D.,Dolle, Roland E.,Shaw, Antony,McNair, David,Novelli, Riccardo,Novelli, Christine E.,Slingsby, Brian P.,Shah, Virendra P.,Tew, David,Saxty, Barbara A.,Allen, Mark,Groot, Pieter H.,Pearce, Nigel,Yates, John
, p. 3569 - 3584 (2007/10/03)
ATP-citrate lyase is the primary enzyme responsible for the synthesis of cytosolic acetyl-CoA in many tissues. Inhibitors of the enzyme represent a potentially novel class of hypolipidemic agent, which are anticipated to have combined hypocholesterolemic and hypotriglyceridemic properties. A series of 2-substituted butanedioic acids have been designed and synthesized as inhibitors of the enzyme. The best compounds, 58, 68, 71, 74 have reversible K(i)'s in the 1-3 μM range against the isolated rat enzyme. As representative of this compound class, 58, has been shown to exert its inhibitory action through a mainly competitive mechanism with respect to citrate and a noncompetitive one with respect to CoA. None of the inhibitors were able to inhibit cholesterol and/or fatty acid synthesis in HepG2 cells. This has been attributed to the adverse physicochemical properties of the molecules leading to a lack of cell penetration. Despite this, a lead structural class of compound has been identified with the potential for modification into potent, cell-penetrant, and efficacious inhibitors of ATP- citrate lyase.
4-(Substituted alkyl)-N-(1,3-dithiolan-2-ylidene(aniline
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, (2008/06/13)
N-(1,3-dithiolan-2-ylidene)-4-alkylanilines having a hydroxy, alkoxy or alkanoyloxy substituent on the alkyl group are useful as anti-inflammatory agents, as analgesic agents and as antiasthmatic agents. The compounds involved can be prepared by the reaction of an appropriate 4-alkylaniline with a methyl(1,3-dithiolan-2-ylidene)sulfonium salt or with carbon disulfide and ethylene dibromide in the presence of a base.
