1027388-49-3Relevant 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.
From metacyclophanes to cyclacenes: Synthesis and properties of [6.8] 3cyclacene
Esser, Birgit,Bandyopadhyay, Arkasish,Rominger, Frank,Gleiter, Rolf
experimental part, p. 3368 - 3379 (2009/12/25)
In this article we show synthetic pathways to [6.8]ncyclacenes demonstrated by the de novo synthesis of [6.8]3cyclacene as the first purely hydrocarbon cyclacene and of precursors for [6.8]4cyclacene. The design of the de
Synthesis of [6.8]3cyclacene: Conjugated belt and model for an unusual type of carbon nanotube
Esser, Birgit,Rominger, Frank,Gleiter, Rolf
, p. 6716 - 6717 (2008/12/22)
[6.8]3Cyclacene as the first hydrocarbon being a fully conjugated molecular belt has been synthesized in an eight-step reaction sequence starting from 4,6-dimethylisophthalaldehyde. It is the smallest and most strained member of the [6.8]cyclacene family, and the synthetic path offers a general route to its higher members. The structural pattern of [6.8]3cyclacene represents a model for a novel type of carbon nanotubes. Copyright
