50892-49-4Relevant articles and documents
Molecular determinants for improved activity at PPARα: Structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARα
Lamers, Christina,Dittrich, Michaela,Steri, Ramona,Proschak, Ewgenij,Schubert-Zsilavecz, Manfred
, p. 4048 - 4052 (2014)
Peroxisome proliferator-activated receptors (PPARs) are attractive targets for the treatment of the metabolic syndrome. Especially a combination of PPARα and PPARγ agonistic activity seems worthwhile to be pursued. Herein we present the design and synthes
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation
Pollinger, Julius,Gellrich, Leonie,Schierle, Simone,Kilu, Whitney,Schmidt, Jurema,Kalinowsky, Lena,Ohrndorf, Julia,Kaiser, Astrid,Heering, Jan,Proschak, Ewgenij,Merk, Daniel
supporting information, p. 2112 - 2126 (2019/03/08)
The fatty acid sensing nuclear receptor families retinoid X receptors (RXRs) and peroxisome proliferator-activated receptors (PPARs) hold therapeutic potential in neurodegeneration. Valuable pleiotropic activities of Wy14,643 in models of such conditions
Molecular determinants for improved activity at PPARα: Structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARα
Lamers, Christina,Dittrich, Michaela,Steri, Ramona,Proschak, Ewgenij,Schubert-Zsilavecz, Manfred
supporting information, p. 4048 - 4052 (2015/03/14)
Peroxisome proliferator-activated receptors (PPARs) are attractive targets for the treatment of the metabolic syndrome. Especially a combination of PPARα and PPARγ agonistic activity seems worthwhile to be pursued. Herein we present the design and synthes
Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition
Hanke, Thomas,Lamers, Christina,Gomez, Roberto Carrasco,Schneider, Gisbert,Werz, Oliver,Schubert-Zsilavecz, Manfred
supporting information, p. 3757 - 3763 (2014/09/17)
The concept of dual PPARα/γ activation was originally proposed as a new approach for the treatment of the metabolic syndrome. However, recent results indicated that PPARα as well as PPARγ activation might also be beneficial in the treatment of inflammator
Design, synthesis, and biological evaluation of a novel class of γ-secretase modulators with pparγ activity
Hieke, Martina,Ness, Julia,Steri, Ramona,Dittrich, Michaela,Greiner, Christine,Werz, Oliver,Baumann, Karlheinz,Schubert-Zsilavecz, Manfred,Weggen, Sascha,Zettl, Heiko
supporting information; experimental part, p. 4691 - 4700 (2010/10/03)
We present a novel class of dual modulators of γ-secretase and peroxisome proliferator-activated receptor γ (PPARγ) based on the structure of 2-(bis(phenethoxy)pyrimidine-2-ylthio)hexanoic acid 8 (IC 50(Aβ42) = 22.8 μM, EC50(PPARγ) =
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARγ modulator
Thieme, Theresa M.,Steri, Ramona,Proschak, Ewgenij,Paulke, Alexander,Schneider, Gisbert,Schubert-Zsilavecz, Manfred
supporting information; scheme or table, p. 2469 - 2473 (2010/07/16)
Peroxisome proliferator-activated receptor γ (PPARγ) is involved in glucose and lipid homeostasis. PPARγ agonists are in clinical use for the treatment of type 2 diabetes. Lately, a new class of selective PPARγ modulators (SPPARγMs) was developed, which are believed to show less side effects than full PPARγ agonists. We have previously shown that α-substitution of pirinixic acid, a moderate agonist of PPARα and PPARγ, leads to low micromolar active balanced dual agonists of PPARα and PPARγ. Herein we present modifications of pirinixic acid leading to subtype-selective PPARγ agonists and furthermore the development of a selective PPARγ modulator guided by molecular docking studies.
Functionalization of fatty acid mimetics for solid-phase coupling and subsequent target identification
Dittrich, Michaela,Zettl, Heiko,Schubert-Zsilavecz, Manfred
scheme or table, p. 625 - 630 (2011/09/14)
Fatty acid mimetics such as pirinixic acid (PA) derivatives and 2-(phenylthio)alkanoic acid derivatives are drug-like small molecules with an interesting pharmacological profile. Previously, we have characterized PA derivatives (e.g., 1) as dual agonists
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase
Koeberle, Andreas,Zettl, Heiko,Greiner, Christine,Wurglics, Mario,Schubert-Zsilavecz, Manfred,Werz, Oliver
supporting information; scheme or table, p. 8068 - 8076 (2009/12/07)
Dual inhibition of the prostaglandin (PG) and leukotriene (LT) biosynthetic pathway is supposed to be superior over single interference, both in terms of efficacy and side effects. Here, we present a novel class of dual microsomal PGE2 synthase
Azoles and azines: CXIX. Alkylation of 5,5′-(4-nitrobenzylidene) bis(2-thiobarbituric) acid and 5-(4-nitrophenyl)-2,8-dithioxo-5,7,8,9- tetrahydro-2H-pyrano[2,3-d:6,5-d′]dipyrimidine-4,6(1H,3H)-dione with haloacetic acids and their esters
Fedorova,Meshcheryakov,Ganina,Moskvin,Ivin
, p. 128 - 133 (2007/10/03)
5,5′-(4-Nitrobenzylidene)bis(2-thiobarbituric) acid and 5-(4-nitrophenyl)-2,8-dithioxo-5,7,8,9-tetrahydro-2H-pyrano[2,3-d:6,5-d′] dipyrimidine-4,6(1H,3H)-dione, similar to unsubstituted 2-thiobarbituric acid, readily react with haloacetic acids and their
ARYLTHIOETHERPYRIMIDINE AND ARYLOXYETHERPYRIMIDINE DERIVATIVES AND THEIR THERAPEUTIC USES
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Page 50, (2008/06/13)
Pyrimidine compounds, compositions containing pyrimidine compounds and methods of using pyrimidine compounds for regulating the production and/or release of ?-amyloid in cells are provided. The compounds provide for alleviation and prevention of ?-amyloid production, release and/or plaque development as occurs in, e.g., Alzheimer's disease.
