- 1,3,5-Trisubstituted aryls as highly selective PPARδ agonists
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A series of highly potent and selective PPARδ agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 μM, making it a useful tool in studying the biological effects of selective PPARδ activation.
- Epple, Robert,Azimioara, Mihai,Russo, Ross,Bursulaya, Badry,Tian, Shin-Shay,Gerken, Andrea,Iskandar, Maya
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p. 2969 - 2973
(2007/10/03)
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- Synthesis and structure-antifungal activity relationships of 3-aryl-5-alkyl-2,5-dihydrofuran-2-ones and their carbanalogues: Further refinement of tentative pharmacophore group
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Two series of 3-(substituted phenyl)-5-alkyl-2,5-dihydrofuran-2-ones related to a natural product, (-)incrustoporine, were synthesized and their in vitro antifungal activity evaluated. The compounds with halogen substituents on the phenyl ring exhibited selective antifungal activity against the filamentous strains of Absidia corymbifera and Aspergillus fumigatus. On the other hand, the influence of the lenghth of the alkyl chain at C(5) was marginal. The antifungal effect of the most active compound against the above strains was higher than that of ketoconazole, and close to that of amphotericin B. In order to verify the hypothesis about a possible relationship between the Michael-accepting ability of the compounds and their antifungal activity, a series of simple carbanalogues, 2-(substituted phenyl)cyclopent-2-enones, was prepared and subjected to antifungal activity assay as well.
- Pour, Milan,Spulak, Marcel,Balsanek, Vojtech,Kunes, Jiri,Kubanova, Petra,Buchta, Vladimir
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p. 2843 - 2866
(2007/10/03)
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- Soluble Substituted μ-Oxo(phthalocyaninato)iron(III) Dimers
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Attempts to prepare various peripheral tetra- and octasubstituted (phthalocyaninato)iron derivatives RnPcFe by starting from the corresponding substituted phthalonitriles led to substituted (μ-oxo)bis compounds 2O.The tert-butyl- and ethyl-substituted systems 2O (6c) and 2O (6d) were reinvestigated.UV/Vis, FD mass, Moessbauer, NMR as well as ESR spectroscopy was used to characterize the complexes 2O to furnish evidence for the presence of Fe-O-Fe moieties in 2O.The UV/Vis data reported for 2O as well as their spectral behavior in pyridine correspond to unsubstituted 2O.Moessbauer spectra of 2O show that the complexes were obatined as a mixtures of two isomeric μ-oxo compounds A (δFe = 0.22 mm s-1, ΔEQ = 1.33-1.39 mm s-1) and B (δFe = 0.33-0.36 mm s-1, ΔEQ = 0.39-0.53 mm s-1), whose Moessbauer parameters are comparable to 2O μ-oxo(2) and μ-oxo(1), respectively.Moessbauer spectral data of 2O indicate high-spin (S = 5/2) FeIII centers.NMR-spectra of 2O (n = 4: R = tBu, Et, O(2-Et-n-C6H13), OCH2C(CH3)2CH2Ph; n = 8: R = O-n-C8H17, O(2-Et-n-C6H13) give further evidence for μ-oxo bridge structures. - Key Words: μ-Oxobis(phthalocyaninato)iron/ μ-Oxo dimers/ Moessbauer spectroscopy/ Iron complexes/ Phthalocyanines
- Dieing, Reinhold,Schmid, Gabriele,Witke, Elisabeth,Feucht, Carola,Dressen, Michael,et al.
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p. 589 - 598
(2007/10/02)
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