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Pharmacological properties of acid N-thiazolylamide FFA2 agonists
FFA2 is a receptor for short‐chain fatty acids. Propionate (C3) and 4‐chloro‐α‐(1‐methylethyl)‐N‐2‐thiazolyl‐benzeneacetamide (4‐CMTB), the prototypical synthetic FFA2 agonist, evoke calciumExpand
Highly chemoselective hydrogenolysis of iodoarenes.
The catalytic hydrodehalogenation reaction using molecular hydrogen and Pd/C has been revisited. It is shown that the speed of removal of halogen increases with increasing electronegativity I < Br <Expand
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds areExpand
α-Sulfonyl Carbanions: Combined Kinetic, Thermodynamic, and NMR Approaches for the Study of the Ionization of Benzyltriflones in Me2SO and H2O−Me2SO Mixtures
The ionization of a series of benzyltriflones ArCH2SO2CF3 (Ar = C6H5, 4-CNC6H4, 4-NO2C6H4, 2,4-(NO2)2C6H3, 2,4,6-(NO2)3C6H2) has been studied kinetically and thermodynamically as well as by 1H, 13C,Expand
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor α agonists
Starting from the structure of 5, a two-step strategy was applied to identify a new generation of trifluoromethane sulfonamides as potent PPARalpha agonists. Synthesis, in vitro and in vivoExpand
Synthesis and DNA binding properties of saturated distamycin analogues.
A series of saturated heterocyclic analogues of distamycin were prepared and examined. A fluorescent intercalator displacement (FID) assay conducted on p[dA]-p[dT] DNA to obtain C(50) values and aExpand
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists.
Identification of indazole derivatives acting as dual angiotensin II type 1 (AT1) receptor antagonists and partial peroxisome proliferator-activated receptor-γ (PPARγ) agonists is described. StartingExpand
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
RIP1 kinase regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including inflammatory and neurological diseases. Currently, RIP1Expand
An isosparteine derivative for stereochemical assignment of stereogenic (chiral) methyl groups using tritium NMR: theory and experiment.
(N-CHDT)-(alpha)-isosparteinium ditosylamide can be used in conjunction with tritium NMR spectroscopy to assign the configuration of an intact stereogenic (chiral) methyl group. The S-CHDT group hasExpand
The discovery of equipotent PPARalpha/gamma dual activators.
We report the design and synthesis of equipotent PPARalpha/gamma dual agonists starting from selective PPAR alpha agonist 1. In vivo data for 7 in the Zucker fa/fa rat are presented.