Search results for "trifluoromethyl"
showing 8 items of 288 documents
Clearance and metabolism of arachidonic acid by C6 glioma cells and astrocytes.
1995
Effects of increased levels of arachidonic acid (AA) were analyzed in vitro by employment of C6 glioma cells and astrocytes from primary culture. The cells were suspended in a physiological medium added with arachidonic acid (AA) in a concentration range from 0.01 to 0.5 mM. The concentration profiles of the fatty acid and AA-metabolites were subsequently followed for 90 min. AA was measured by gas chromatography, whereas the AA-metabolites PGF2 alpha and LTB4 by radioimmunoassay (RIA). Following administration of AA at 0.05 or 0.1 mM the medium was completely cleared from the fatty acid within 10 to 15 min. However, when 0.5 mM were added, AA concentrations of 0.36 +/- 0.055 mM were found …
Effects of endothelin-1 on the cerebrovascular bed of the goat.
1991
Abstract The aim of the present study was to analyze the effects of endothelin-1 (ET-1) in the cerebrovascular bed of the goat, the importance of endothelial integrity and the contribution of extracellular Ca2+ to these responses. We measured isometric tension and 45Ca2+ uptake in isolated middle cerebral arteries, and cerebral blood flow (CBF) in unanesthetized animals. ET-1 elicited concentration-dependent contractions which were potentiated in arteries without endothelium. Ca2+-free medium and nicardipine inhibited, and Bay K 8644 potentiated the ET-1-induced contractions. ET-1 enhanced 45Ca2+ uptake in isolated arteries. Injections of ET-1 directly into the cerebral circulation decrease…
Synthesis and Molecular Modeling Studies of Derivatives of a Highly Potent Peptidomimetic Vinyl Ester as Falcipain-2 Inhibitors
2012
Herein we report the synthesis of a set of constrained peptidomimetics endowed with an electrophilic vinyl ester warhead and structurally related to a previously identified lead compound, a potent and irreversible inhibitor of falcipain-2 (FP-2). FP-2 is the main hemoglobinase of the malaria parasite P. falciparum. The new compounds were evaluated for their inhibition against FP-2, and the results were rationalized on the basis of docking experiments. These studies underscore the pivotal role of both the ester function at the P1' site and the trifluoromethyl group of the P3 side chain in determining the correct orientation of the Michael acceptor warhead in the catalytic site, and as a cons…
CCDC 953883: Experimental Crystal Structure Determination
2013
Related Article: Huayan Yang, Yu Wang, Huaqi Huang, Lars Gell, Lauri Lehtovaara, Sami Malola, Hannu Hakkinen, Nanfeng Zheng|2013|Nat.Commun.|4|2422|doi:10.1038/ncomms3422
CCDC 1020496: Experimental Crystal Structure Determination
2014
Related Article: Huayan Yang , Yu Wang , Juanzhu Yan , Xi Chen , Xin Zhang , Hannu Häkkinen , and Nanfeng Zheng|2014|J.Am.Chem.Soc.|136|7197|doi:10.1021/ja501811j
Organocatalytic Enantioselective Vinylogous Henry Reaction of 3,5-Dimethyl-4-nitroisoxazole with Trifluoromethyl Ketones
2017
The enantioselective vinylogous Henry reaction of 3,5-dimethyl-4-nitroisoxazole with trifluoromethyl ketones employing a bifunctional squaramide organocatalyst has been developed. A series of isoxazole bearing trifluoromethyl-substituted tertiary alcohols, 2-substituted (R)-1,1,1-trifluoro-3-(3-methyl-4-nitroisoxazol-5-yl)propan-2-ols, were obtained under these mild reaction conditions in good yields and moderate to good enantioselectivities
CCDC 1448944: Experimental Crystal Structure Determination
2017
Related Article: Francis A. LeBlanc, Andreas Decken, T. Stanley Cameron, Jack Passmore, J. Mikko Rautiainen, and Thomas K. Whidden|2017|Inorg.Chem.|56|974|doi:10.1021/acs.inorgchem.6b02670
CCDC 1573313: Experimental Crystal Structure Determination
2017
Related Article: Niklas Struch, Filip Topic, Gregor Schnakenburg, Kari Rissanen, Arne Lützen|2018|Inorg.Chem.|57|241|doi:10.1021/acs.inorgchem.7b02412