- Oxime Carbamate-Discovery of a series of novel FAAH inhibitors
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A series of novel oxime carbamates have been identified as potent inhibitors of the key regulatory enzyme of the endocannabinoid signaling system, fatty acid amide hydrolase (FAAH). In this Letter, the rationale behind the discovery and the biological evaluations of this novel class of FAAH inhibitors are presented. Both in vitro and in vivo results of selected targets are discussed, along with inhibition kinetics and molecular modeling studies.1.
- Sit,Conway, Charles M.,Xie, Kai,Bertekap, Robert,Bourin, Clotilde,Burris, Kevin D.
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supporting information; experimental part
p. 1272 - 1277
(2010/06/17)
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- Heterocyclic analogs of prostaglandines: IV. Synthesis of 3,7-interphenylene 3,10(11)-dioxa-13-azaprostanoids and 9-oxa-7-azaprostanoids based on tetronic acid and aromatic aldehydes
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An approach was developed to the synthesis of stable in metabolism 3,7-interphenylene 3,10-dioxa-13-aza-and 3,11-dioxa-13-azaprostanoids, and also 9-oxa-7-azaprostanoids with interphenylene and terminal phenyl fragments in the ω-chain based on 3-(alkoxybenzylidene)-and 3-(3-phenylallylidene) tetrahydrofuran-2,4-diones obtained by Knoevenagel condensation of tetronic acid with alkoxy-substituted aromatic aldehydes and cinnamic aldehyde.
- Pashkovskii,Shchukina,Gribovskii,Lakhvich
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experimental part
p. 657 - 670
(2009/04/07)
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- Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
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The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.
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- Synthesis and thermal properties of cholesteryl 4-n-alkoxy-3-methoxybenzoates
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A homologous series of new liquid crystalline compounds, cholesteryl 4-n-alkoxy-3-methoxybenzoate were synthesized from vanillin and their mesomorphic properties were studied by differential scanning calorimetry, polarizing microscopy and x-ray diffractometry.Each of the homologues from cholesteryl 3,4-dimethoxybenzoate (n=1) to cholesteryl 4-n-hexyloxy-3-methoxybenzoate (n=6) showed a cholesteric-nematic phase (NCh).The other higher homologues (from n=7 to n=18) indicated smectic A (SA) and NCh phases.The temperature region of smectic phases increased with the increase of the chain length of the n-alkoxy group.Transition temperatures in each of the homologues were lower than those in a corresponding non-3-methoxy substituted benzoate ester, due to the destabilizing effect of the lateral methoxy group.The effect was more significant on the homologues having a shorter n-alkoxy chain.It was also found that these esters formed a glassy state by quenching from mesophases and/or the isotropic liquid phase.The change of the glass transition temperature on each homologue (from n=1 to n=6) suggested the effect of the chain length of the n-alkoxyl group on the formation of the glassy state.Keywords: liquid crystals, thermal properties, differential scanning calorimetry, cholesteric phas, smectic A phase, glassy phase.
- Kasuga, Kazuyuki,Hatakeyama, Hyoe,Hatakeyama, Tatsuko
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