263716-00-3Relevant articles and documents
Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes
Baskakis, Constantinos,Magrioti, Victoria,Cotton, Naomi,Stephens, Daren,Constantinou-Kokotou, Violetta,Dennis, Edward A.,Kokotos, George
experimental part, p. 8027 - 8037 (2009/11/30)
The development of selective inhibitors for individual PLA2 enzymes is necessary in order to target PLA2-specific signaling pathways, but it is challenging due to the observed promiscuity of known PLA2 inhibitors. In the current work, we present the development and application of a variety of synthetic routes to produce pentafluoro, tetrafluoro, and trifluoro derivatives of activated carbonyl groups in order to screen for selective inhibitors and characterize the chemical properties that can lead to selective inhibition. Our results demonstrate that the pentafluoroethyl ketone functionality favors selective inhibition of the GVIA iPLA2, a very important enzyme for which specific, potent, reversible inhibitors are needed. We find that 1,1,1,2,2-pentafluoro-7-phenyl-heptan-3-one (FKGK11) is a selective inhibitor of GVIA iPLA2 (XI(50) = 0.0073). Furthermore, we conclude that the introduction of an additional fluorine atom at the α′ position of a trifluoromethyl ketone constitutes an important strategy for the development of new potent GVIA iPLA2 inhibitors.
Chiral compounds
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, (2008/06/13)
The invention relates to chiral compounds of formula I wherein R1, R2, X, Y1and Y2have the meanings defined herein, as well as to liquid crystalline mixtures comprising at least one chiral compound of formula I. The invention also relates to chiral linear or crosslinked liquid crystalline polymers obtainable by polymerizing a polymerizable mixture comprising at least one chiral compound of formula I, and to the use of chiral compounds of formula I and mixtures and polymers obtained thereof in liquid crystal displays, such as STN, TN, AMD-TN, temperature compensation, guest-host, phase change or surface stabilized or polymer stabilized cholesteric texture (SSCT, PSCT) displays, in active and passive optical elements like polarizers, compensators, alignment layers, color filters or holographic elements in adhesives, synthetic resins with anisotropic mechanical properties, cosmetics, diagnostics, liquid crystal pigments, for decorative and security applications, in nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula I.
Non-chiral compounds exhibiting alternating tilt smectic phases
Tuffin,Goodby,Bennemann,Heppke,Loetzsch,Scherowsky
, p. 51 - 67 (2007/10/02)
In this article we present an investigation of the liquid crystal properties of non-chiral and racemic branched alkyl chain (swallow-tailed) molecules and some chiral analogues based on a cinnamic acid core group. It was found in these systems that increasing the extent of the branching of the terminal alkyl chain increased the incidence of alternating tilt smectic phases, whereas smectic Cα and smectic Cγ phases were suppressed. X-ray studies of the effect on the layer spacing in the smectic A phase of increasing the long alkyl branch of one series of compounds are included. Results of polarisation studies on some chiral analogues are also reported.
