25445-41-4Relevant academic research and scientific papers
Synthesis and biological evaluation of dihydropyrano-[2,3-c]pyrazoles as a new class of PPAR? partial agonists
Qvortrup, Katrine,Jensen, Jakob F.,S?rensen, Mikael S.,Kouskoumvekaki, Irene,Petersen, Rasmus K.,Taboureau, Olivier,Kristiansen, Karsten,Nielsen, Thomas E.
, (2017/03/09)
Peroxisome proliferator-activated receptor ? (PPAR?) is a well-known target for thiazolidinedione antidiabetic drugs. In this paper, we present the synthesis and biological evaluation of a series of dihydropyrano[2,3-c]pyrazole derivatives as a novel family of PPAR? partial agonists. Two analogues were found to display high affinity for PPAR? with potencies in the micro molar range. Both of these hits were selective against PPAR?, since no activity was measured when tested against PPARα, PPAR? and RXRα. In addition, a novel modelling approach based on multiple individual flexible alignments was developed for the identification of ligand binding interactions in PPAR?. In combination with cell-based transactivation experiments, the flexible alignment model provides an excellent analytical tool to evaluate and visualize the effect of ligand chemical structure with respect to receptor binding mode and biological activity.
Solid-state diphotocyclization of iso- and terephthalaldehydes via dihalogen substitution
Moorthy, J. Narasimha,Venkatakrishnan,Mal, Prasenjit,Venugopalan
, p. 327 - 330 (2007/10/03)
The supramolecular nonbonded C-H···X interactions between formyl hydrogens and ortho-halogen atoms (Br/Cl) have been exploited to achieve conformational control in the solid state of dimethyl-substituted iso- and terephthaladehydes (1-3) for unprecedented
Formylation and dichloromethylation as alternative directions of rieche reaction. A novel to the synthesis of sterically hindered aromatic dialdhydes
Yakubov, Alexander P.,Tsyganov, Dmitry V.,Belen'kii, Leonid I.,Krayushkin, Mikhail M.
, p. 3397 - 3404 (2007/10/02)
A previously unknown direction of Rieche reaction has been found: formylation of mesitylene, m-xylene, and durene with dichloromethyl methyl ether in the presence of aluminium trichloride and, to lesser extent, of titanium tetrachloride give the respective benzylidene dichlorides besides aldehydes. A novel approach to the synthesis of sterically hindered aromatic dialdehydes has been offered which involves the transformation of a monoaldehyde into the corresponding benzylidene dichloride, Rieche formylation of the latter, and hydrolysis of dichloromethyl aldehyde formed.
Vilsmeier-Haack Reaction on Some 3-Buten-2-ols
Sreenivasulu, M.,Krishna Rao, G.S.
, p. 1187 - 1188 (2007/10/02)
Vilsmeier-Haack reaction on 3-buten-2-ols (1b-i) leads to benzene mono-, di- and tricarboxaldehyde (3-8) in yields ranging from 6-26percent.The presence of at least five appropriate participating carbon atoms on the butenol backbone (1b-n) seems to be essential for formylative benzocyclization to occur.
