Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Pavel Pihera"'
Publikováno v:
Tetrahedron Letters. 48:6970-6973
Allylic thioethers of the general structure 1 underwent E / Z isomerization during both basic and acidic hydrolysis of the ester moiety at the remote end of the molecule. The isomerization was dependent on the substitution of the allylic moiety. The
Autor:
Claus Bekker Jeppesen, Per Sauerberg, Eva Johansson, Marek Korínek, Miroslav Havranek, Søren Ebdrup, John Patrick Mogensen, Pavel Pihera, Ingrid Pettersson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4625-4629
Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdel
Autor:
Jan Fleckner, Zdenek Polivka, Erik M. Wulff, John Patrick Mogensen, Pavel Pihera, Miroslav Havranek, Claus Bekker Jeppesen, Paul Stanley Bury, Per Sauerberg, Lone Jeppesen, Grith Skytte Olsen, Ingrid Pettersson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3198-3202
Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARα agonists. Optimum PPARα potency and selectivity were obtained with substituents having van der Waals volume around 26
Autor:
Miroslav Havranek, Vladimira Panajotova, Zdenek Polivka, Pavel Pihera, Ingrid Pettersson, Jens R. Daugaard, Lone Jeppesen, Elisabeth D. Galsgaard, Grith Skytte Olsen, Lars Ynddal, Erik M. Wulff, John Patrick Mogensen, Jan Fleckner, Claus Bekker Jeppesen, Per Sauerberg
Publikováno v:
Journal of Medicinal Chemistry. 50:1495-1503
The aim was to identify a novel selective PPARdelta agonist with full efficacy on free fatty acid (FFA) oxidation in vitro and plasma lipid correction in vivo. Using the triple PPARalpha,gamma,delta agonist 1 as the structural starting point, we want
Publikováno v:
Scopus-Elsevier
A new synthesis of the title compound based on the formation of the furan ring in the key step was elaborated. Methyl 2-methoxy[1]benzothieno[3,2-b][1]benzofuran-7-carboxylate (15) was prepared by this methodology as a new type of a core for liquid c
Autor:
Pavel Pihera, Jiri Svoboda
Publikováno v:
Collection of Czechoslovak Chemical Communications. 65:58-76
Electrophilic substitution and metallation reactions of the title compound 1 were studied. Bromination, acetylation, benzoylation, formylation, and nitration usually afforded nonseparable mixtures of 2- and 7-substituted derivatives as the main produ
Publikováno v:
Collection of Czechoslovak Chemical Communications. 64:389-407
2-Vinyl- (2) and 3-vinyl[1]benzothieno[3,2-b]furan (3) react with dimethyl acetylenedicarboxylate, methyl propiolate, maleic anhydride, or acrylonitrile endo-selectively as dienes to afford new [1]benzothieno[3,2-b][1]benzofuran derivatives 7-20. cis
Publikováno v:
Collection of Czechoslovak Chemical Communications. 63:681-697
[1]Benzothieno[3,2-b]furan reacts with substituted dienes 2 as a dienophile under formation of substituted tetrahydro[1]benzothieno[3,2-b][1]benzofuran derivatives 3-14. The cycloaddition is endo-stereoselective. Aromatization of the products leads t
Publikováno v:
Collection of Czechoslovak Chemical Communications. 62:1468-1480
Thieno[3,2-b]benzofuran was synthesized starting from benzo[b]furan-3(2H)-one or benzo[b]furan-2-carbaldehyde. Electrophilic substitution reactions such as bromination, formylation, acetylation or nitration, take place in position 2. An electron dona
Publikováno v:
Collection of Czechoslovak Chemical Communications. 61:888-900
In chlorination, bromination, iodination, nitration, sulfonation, formylation, and trifluoroacetylation of [1]benzothieno[3,2-b]furan (1) the substituent enters the 2-position. The said halogenations go by the addition-elimination mechanism. When the