64460-85-1Relevant academic research and scientific papers
Structural optimization and in vitro profiling of N-phenylbenzamide-based farnesoid X receptor antagonists
Schmidt, Jurema,Schierle, Simone,Gellrich, Leonie,Kaiser, Astrid,Merk, Daniel
, p. 4240 - 4253 (2018/07/21)
Activation of the nuclear farnesoid X receptor (FXR) which acts as cellular bile acid sensor has been validated as therapeutic strategy to counter liver disorders such as non-alcoholic steatohepatitis by the clinical efficacy of obeticholic acid. FXR antagonism, in contrast, is less well studied and potent small molecule FXR antagonists are rare. Here we report the systematic optimization of a novel class of FXR antagonists towards low nanomolar potency. The most optimized compound antagonizes baseline and agonist induced FXR activity in a full length FXR reporter gene assay and represses intrinsic expression of FXR regulated genes in hepatoma cells. With this activity and a favorable toxicity-, stability- and selectivity-profile it appears suitable to further study FXR antagonism in vitro and in vivo.
Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening
Borthwick, Jennifer A.,Ancellin, Nicolas,Bertrand, Sophie M.,Bingham, Ryan P.,Carter, Paul S.,Chung, Chun-Wa,Churcher, Ian,Dodic, Nerina,Fournier, Charlène,Francis, Peter L.,Hobbs, Andrew,Jamieson, Craig,Pickett, Stephen D.,Smith, Sarah E.,Somers, Donald O'N.,Spitzfaden, Claus,Suckling, Colin J.,Young, Robert J.
, p. 2452 - 2467 (2016/04/10)
Inhibitors of mitochondrial branched chain aminotransferase (BCATm), identified using fragment screening, are described. This was carried out using a combination of STD-NMR, thermal melt (Tm), and biochemical assays to identify compounds that b
Solvent-Free Selective Hydrogenation of Nitroarenes Using Nanoclusters of Palladium Supported on Nitrogen-Doped Ordered Mesoporous Carbon
Huang, Haigen,Wang, Xueguang,Tan, Mingwu,Chen, Chenju,Zou, Xiujing,Ding, Weizhong,Lu, Xionggang
, p. 1485 - 1489 (2016/05/02)
The selective hydrogenation of nitroarenes is a key transformation for the production of aromatic amines, which are primary intermediates in the synthesis of pharmaceuticals, agrochemicals, and dyes. However, most reaction processes require toxic organic solvents and suffer from poor selectivity in the presence of other reducible groups. Herein, we report a successful example of nanoclusters of ultrafine Pd supported on N-modified ordered mesoporous CMK-3 carbon (Pd/N-CMK-3) prepared by a facile two-step impregnation route with aqueous solutions of 1,10-phenanthroline and H2PdCl4 that hydrogenated various nitroarenes highly efficiently and selectively to the corresponding aromatic amines with hydrogen in the absence of solvent. The Pd/N-CMK-3 catalyst could be recovered easily for multiple recycling reactions without a loss of catalytic performance.
METHOD FOR TREATING VIRUS INFECTION USING DERIVATIVE OF ANILINE
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, (2015/07/15)
A method for treating a virus infection in a subject is provided. The method comprising administering to the subject in need an effective amount of a derivative of aniline selected from the group consisting of a compound of formula (I), a pharmaceutically
ANTIVIRAL COMPOUNDS
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Paragraph 0246; 0247; 0248; 0349, (2013/08/28)
The present invention provides new antiviral compounds and pharmacological compositions comprising these new compounds and their use in the prophylaxis, prevention and treatment of viral infections, particularly adenovirus and herpes virus infections.
Synthesis, biological evaluation, and structure-activity relationships of 2-[2-(benzoylamino)benzoylamino]benzoic acid analogues as inhibitors of adenovirus replication
?berg, Christopher T.,Strand, M?rten,Andersson, Emma K.,Edlund, Karin,Tran, Nam Phuong Nguyen,Mei, Ya-Fang,Wadell, G?ran,Elofsson, Mikael
experimental part, p. 3170 - 3181 (2012/06/04)
2-[2-Benzoylamino)benzoylamino]benzoic acid (1) was previously identified as a potent and nontoxic antiadenoviral compound (Antimicrob. Agents Chemother. 2010, 54, 3871). Here, the potency of 1 was improved over three generations of compounds. We found that the ortho, ortho substituent pattern and the presence of the carboxylic acid of 1 are favorable for this class of compounds and that the direction of the amide bonds (as in 1) is obligatory. Some variability in the N-terminal moiety was tolerated, but benzamides appear to be preferred. The substituents on the middle and C-terminal rings were varied, resulting in two potent inhibitors, 35g and 35j, with EC50 = 0.6 μM and low cell toxicity.
NEW ANTIVIRAL COMPOUNDS
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Page/Page column 42; 56, (2012/01/05)
The present invention provides new antiviral compounds and pharmacological compositions comprising these new compounds and their use in the prophylaxis, prevention and treatment of viral infections, particularly adenovirus and herpes virus infections.
Thrombin inhibitors
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Page 19, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.
CONDENSED INDOLE DERIVATIVES AS 5HT4-RECEPTOR ANTAGONISTS
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, (2008/06/13)
Compounds of formula (I) and pharmaceutically acceptable salts thereof: STR1 and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
Condensed indole derivatives as 5HT4 -receptor antagonists
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, (2008/06/13)
Compounds of formula (I) and pharmaceutically acceptable salts thereof: STR1 and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
