64460-85-1Relevant articles and documents
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.
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.
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.