86688-96-2Relevant academic research and scientific papers
Design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3β inhibitors
Ye, Qing,Li, Meng,Zhou, Yu-Bo,Cao, Jia-Yu,Xu, Lei,Li, Yu-Jin,Han, Liang,Gao, Jian-Rong,Hu, Yong-Zhou,Li, Jia
, p. 349 - 358 (2013/07/19)
A series of 3-aryl-4-pyrrolyl-maleimides were designed, synthesized, and evaluated for their glycogen synthase kinase-3β (GSK-3β) inhibitory activity. Most compounds exhibited potent activity against GSK-3β. Among them, compounds 11a, 11c, 11h, 11i, and 11j significantly reduced Aβ-induced Tau hyperphosphorylation, showing the inhibition of GSK-3β at the cellular level. Structure-activity relationships were discussed based on the experimental data obtained. Most compounds in a new series of 3-aryl-4-pyrrolyl-maleimides exhibited potent glycogen synthase kinase-3β (GSK-3β) inhibitory activity. Compounds 11a, 11c, 11h, 11i, and 11j reduced Aβ-induced Tau hyperphosphorylation, showing inhibition of GSK-3β at the cellular level. Copyright
Synthesis of novel pyrrolyl-indomethacin derivatives
Serra Moreno, Judith,Agas, Dimitrios,Sabbieti, Maria Giovanna,Di Magno, Matteo,Migliorini, Antonella,Loreto, M. Antonietta
, p. 391 - 397 (2013/01/15)
In the present work, we report the synthesis of the novel esters of indomethacin (IDMC) and an ester of reduced IDMC. For this purpose, IDMC is covalently bound by using a spacer chain to the pyrrole (Py) in the 3-position. The innovative pyrrole-indomethacin (3-Py-IDMC) derivates show no cytotoxic effects in primary calvarial osteoblasts. The designed IDMC derivates have been studied because they could be injected locally as a component of polymeric micro-particles. In fact, the new 3-Py-IDMC derivatives will assure their further polymerization since the 2- and 5-monomer positions are free.
Superhydrophobic surfaces of electrodeposited polypyrroles bearing fluorinated liquid crystalline segments
Darmanin, Thierry,De Givenchy, Elisabeth Taffin,Guittard, Frederic
, p. 9365 - 9370 (2011/11/30)
Two intrinsic properties of fluorinated tails (F-butyl to F-octyl) were combined in the elaboration of superhydrophobic surfaces by electrochemical polymerization: their promesogenic characteristic and their ability to increase both hydrophobicity and oleophobicity. We report the synthesis and the characterization of pyrrole monomers bearing fluorinated liquid crystalline segments. The electrodeposited corresponding polymer films were characterized by cyclic voltammetry, static and dynamic contact angle measurements, and scanning electron microscopy. Sticky superhydrophobic surfaces were obtained with a F-hexyl or a F-octyl tail. The presence of mesogenic segments improves the surface hydrophobicity and increases the surface roughness, clearly observed with F-butyl and F-hexyl chains.
Synthesis and polymerization of 2-(3-pyrrolyl)acetic acid derivatives from pyrrole
Ho-Hoang, Ahn,Fache, Fabienne,Lemaire, Marc
, p. 1289 - 1304 (2007/10/03)
The synthesis of the 3-pyrrylacetic acid as well as the study of its esterification conditions are described. The new materials thus obtained are electropolymerized.
Poly[(3-pyrrolyl)acetic acid]
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, (2008/06/13)
A poly[(3-pyrrolyl)acetic acid] is here disclosed which is represented by the formula (I) STR1 wherein n is an integer of 2 or more. This polymer can be prepared by subjecting (3-pyrrolyl)acetic acid to electrolytic oxidation polymerization in the presenc
Regioselective Synthesis of Acylpyrroles
Kakushima, Masatoshi,Hamel, Pierre,Frenette, Richard,Rokach, Joshua
, p. 3214 - 3219 (2007/10/02)
The regioselective synthesis of several pyrrole derivatives is described.AlCl3-catalyzed acylation reactions of 1-(phenylsulfonyl)pyrrole (1) give 3-acyl derivatives, whereas the corresponding BF3*OEt2-catalyzed reactions give 2-acyl derivatives predominantly.Mild alkaline hydrolysis gives the corresponding acyl-1H-pyrroles in excellent yields.AlCl3-catalyzed reactions of 1 with 1,1-dichloromethyl methyl ether and oxalyl chloride give 1-(phenylsulfonyl)-2-formylpyrrole (6) and 1-(phenylsulfonyl)-2-(chlorocarbonyl)pyrrole (7), respectively. 3-Pyrrolylacetic acid (10) was prepared by thallium(III) nitrate promoted rearrangement of 1-(phenylsulfonyl)-3-acetylpyrrole (2a).Trifluoroacetic anhydride catalyzed cyclization of 4-butyric acid (14) gives 1-(phenylsulfonyl)-7-oxo-4,5,6,7-tetrahydroindole (17).Attempts to cyclize 14 at the 4-position have been unsuccessful.
