ABSTRACT
Ten 1,4-disubstituted 1,2,3-triazoles 2a-2j were prepared and tested for their ability to increase oleic acid oxidation in human myotubes using a high-throughput multiwell assay. Compounds 2e (2-{4-[(1-(3-fluoro-4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methylthio]-2-methylphenoxy}acetic acid) and 2i (2-{4-[(1-(3-chloro-4-(trifluoromethoxy)phenyl)-1H-1,2,3-triazol-4-yl)methylthio]-2-methylphenoxy}acetic acid) exhibited potent agonist activities. Compounds 2e and 2i also exhibited powerful agonist effects for both PPARalpha and PPARdelta in a luciferase-based assay. Consequently, these triazoles can be categorized as dual PPAR agonists.
Subject(s)
PPAR alpha/agonists , PPAR delta/agonists , Thiazoles/chemistry , Triazoles/chemistry , Triazoles/pharmacology , Animals , COS Cells , Chlorocebus aethiops , Humans , Triazoles/chemical synthesisABSTRACT
A novel amphiphilic GdPCTA-[12] derivative has been prepared. The complex formed micelles in aqueous solution with a relatively low CMC, 0.15 mM (25 degrees C). The concentration dependent T1-relaxivity (r1) of the system has been described. The maximum T1-relaxivity, 29.2 s-1 mM-1 (20 MHz, 25 degrees C), was higher than for previously described micellar MRI contrast agents. This high T1-relaxivity is a consequence of the favourable water residence time (tau M) and the fact that the complex is heptadentate allowing two water molecules to coordinate to the gadolinium ion (q = 2).
Subject(s)
Contrast Media/chemical synthesis , Gadolinium DTPA/chemical synthesis , Magnetic Resonance Imaging , Micelles , Solutions , Surface-Active Agents/chemical synthesis , WaterABSTRACT
A novel Gd(III) complex, GdDOTA-(BOM)4, has been prepared by a simple three-step procedure. The complex showed high T1-relaxivity values in serum albumin solutions, blood and plasma, resulting from high affinity for serum albumin. The T1-relaxivity in plasma, 67.4 s-1 mM-1 (20 MHz, 37 degrees C), makes it a promising candidate for angiographic applications of MRI.
Subject(s)
Contrast Media/chemical synthesis , Contrast Media/metabolism , Gadolinium/chemistry , Organometallic Compounds/blood , Organometallic Compounds/chemical synthesis , Angiography/methods , Animals , Cattle , Contrast Media/chemistry , Heterocyclic Compounds, 1-Ring/chemistry , Humans , Magnetic Resonance Imaging/methods , Organometallic Compounds/chemistry , Protein Binding , Serum Albumin, Bovine/metabolismABSTRACT
The resin of Commiphora kwo yielded two new octanordammarane triterpenes namely 15 alpha-hydroxymansumbinone and 28-acetoxy-15 alpha-hydroxymansumbinone, along with the four known compounds, mansumbinone, mansumbinol, (16S, 20R)-dihydroxydammar-24-en-3-one and T-cadinol. These structures were elucidated by spectroscopic techniques, including 1D and 2D NMR spectroscopy, and X-ray analysis.
