464190-32-7Relevant academic research and scientific papers
SAR of benzoylpyridines and benzophenones as p38α MAP kinase inhibitors with oral activity
Revesz, Laszlo,Blum, Ernst,Di Padova, Franco E.,Buhl, Thomas,Feifel, Roland,Gram, Hermann,Hiestand, Peter,Manning, Ute,Rucklin, Gerard
, p. 3601 - 3605 (2004)
Benzoylpyridines and benzophenones were synthesized and evaluated in vitro as p38α inhibitors and in vivo in several models of rheumatoid arthritis. Oral activity was found to depend upon substitution: 1,1-dimethylpropynylamine substituted benzophenone 10b (IC50: 14nM) and pyridinoyl substituted benzimidazole 17b (IC50: 21nM) showed highest efficacy and selectivity with ED50s of 9.5 and 8.6mg/kg po in CIA.
Compound, organic light-emitting device, and electronic device
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Paragraph 0158-0161, (2020/05/01)
The invention belongs to the technical field of organic materials, and provides a compound with a structure as shown in a chemical formula 1 which is described in the specification. In the chemical formula 1, Ar1, Ar2, Ar3 and Ar4 are H or a group as shown in a chemical formula 1-1, and at least one of Ar1, Ar2, Ar3 and Ar4 is the group as shown in the chemical formula 1-1. As the molecular structure of the compound contains a triarylamine group, and contains an electron-donating triphenylamine part and a molecular large conjugated system, the molecule of the compound has the property of intramolecular charge transfer. An organic light-emitting device prepared from the compound has high device efficiency. Compared with the prior art, an organic electroluminescent material disclosed by theinvention has higher stability, so the service life of an organic electroluminescent device is prolonged. In addition, a phenanthrene fused ring derivative is used for structural modification of an electron donor and an electron acceptor respectively, so the photophysical and electrochemical properties of the material can be effectively regulated and controlled, and a luminescent layer material with a narrow energy level band gap is obtained. The invention further provides the organic light-emitting device and an electronic device.
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands
Song, Kwang-Seop,Lee, Sung-Han,Chun, Hyun Ji,Kim, Jong Yup,Jung, Myung Eun,Ahn, Kwangwoo,Kim, Soo-Un,Kim, Jeongmin,Lee, Jinhwa
, p. 4035 - 4051 (2008/09/21)
After the CB1 receptor antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Several series of urea, carbamate, amide, sulfonamide and oxalamide derivatives based on 1-benzhydrylpiperazine scaffold were synthesized and tested for CB1 receptor binding affinity. The SAR studies to optimize the CB1 binding affinity led to the potent urea derivatives. After the additional SAR studies to optimize the substituents of diphenyl rings, the combination of 2-chlorophenyl and 4-chlorophenyl turned out to be the most potent scaffold. The CB2 binding affinity assay as well as functional assay was also conducted on these compounds. Herein we wish to introduce several novel CB1 antagonists with IC50 values less than 100 nM for the CB1 receptor binding.
