28547-32-2Relevant academic research and scientific papers
Synthesis and Evaluation of 2-Azetidinone and 1H-Pyrrole-2,5-dione Derivatives as Cholesterol Absorption Inhibitors for Reducing Inflammation Response and Oxidative Stress
Xia, Yineng,Zhu, Lijuan,Yuan, Xinrui,Wang, Yubin
, (2019)
Excess lipid accumulation can initiate the development and progression of atherosclerotic lesions, thus eventually leading to cardiovascular disease. Lipid-lowering medication therapy is one of the cornerstones of cardiovascular disease therapy. On the basis of the cholesterol absorption inhibitor ezetimibe, we successfully synthesized seven 2-azetidinone derivatives and eighteen 1H-pyrrole-2,5-dione derivatives. Most of the new compounds significantly inhibited cholesterol uptake in vitro. In addition, one of the most active inhibitors, 3-(4-fluorophenyl)-1-[(3S)-3-hydroxy-3-(4-hydroxyphenyl)propyl]-4-(4-hydroxyphenyl)-1H-pyrrole-2,5-dione (14q), showed no cytotoxicity in L02 and HEK293T cell lines. Further evaluation indicated that 14q inhibited considerably the amount of TNF-α, ROS, MDA, and LDH in vitro. Therefore, 14q might be a novel cholesterol absorption inhibitor.
SCHWEFELVERBINDUNGEN DES ERDOELS XXII. ALKYL-10,11-DIHYDRODIINDENOTHIOPHENE
Boberg, Friedrich,Deters, Karin,Schulz, Juergen,Torges, Karl-Franz
, p. 69 - 80 (2007/10/03)
The one-pot syntheses of alkyl-10,11-dihydrodiindenothiophenes (3) by bromination and sulfurization of alkylindan-1-ones without substituents at C-2 (1) has been studied with 14 1 with C1-C4-rests at the benzene and or the cyclopentane ring. 9 dialkyl-3 and 3 tetraalkyl-3 are prepared in yields of 7-66percent; an octamethyl-3 is detected by tlc and ms. 2 dialkyl-3 are prepared too by an independent syntheses from dimethyl 2,5-bis(methylphenyl)thiophene-3,4-dicarboxylates (13).The mechanism of the one-pot syntheses, which gives diindeno-1,4-dithiines too,is discussed.The oxidation of 4 3 has been studied.Key words: Alkylindan-1-ones, alkyl-10,11-dihydrodiindenothiophenes, alkyldiindeno-1,4-dithiines, one-pot syntheses of anellated thiophenes, oxidation of anellated thiophenes.
