79294-58-9Relevant academic research and scientific papers
NORVALINE DERIVATIVE AND METHOD FOR PREPARATION THEREOF
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Page/Page column 27; 53, (2008/06/13)
Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of said compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2). [wherein X is -CH2-, -O-, -S- or single bond; Ar is optionally substituted aryl or lower cycloalkyl; n is 0 to 2; R1 and R2 are (i) each is hydrogen or lower alkyl; (ii) R1 and R2 are combined to form lower alkylene; or (iii) R1 is hydrogen or lower alkyl and R2 is combined with R4 or R6 to form lower alkylene; R3 and R4 are (i) each is hydrogen or lower alkyl; (ii) R3 and R4 are combined to form lower alkylene; or (iii) R3 is hydrogen or lower alkyl and R4 is combined with R2 or R6 to form lower alkylene; R is or -OR7; R 5 and R6 are (i) each is optionally substituted lower alkyl, or hydrogen; (ii) R5 and R6 are combined to form aliphatic 5- to 6-membered heterocyclic group; or (iii) R5 is optionally substituted lower alkyl or hydrogen and R6 is combined with R2 or R4 to form lower alkylene; R7 is lower alkyl.
Development of a Novel Series of Trialkoxyaryl Derivatives as Specific and Competitive Antagonists of Platelet Activating Factor
Sawyer, David A.,Beams, Richard M.,Blackwell, Geoffrey, J.,Brockwell, Michael A.,Cheesman, Neil J.,et al.
, p. 2130 - 2137 (2007/10/02)
The synthesis and structure-activity relationship (SAR) analysis of a novel series of trialkoxyaryl derivatives as specific and competetive inhibitors of platelet activating factor (PAF), are described.Molecular modeling comparisons of PAF with the known antagonists Ginkgolide B and L-652731 led to the selection of N-ethyl>-N,N,N-trimethylammonium iodide (1) from the Wellcome registry of compounds and to the synthesis of the lead compound N-oxy>ethyl>-N,N,N-trimethylammonium iodide (3, pKb 5.43).Furth er SAR considerations directed the design to 2-(hexyloxy)-1,3-dimethoxy-5-benzene (38) (pKb 7.14), a novel, specific, and competitive inhibitor of the PAF receptor in rabbit-washed platelets.
Synthesis and thermal properties of cholesteryl 4-n-alkoxy-3-methoxybenzoates
Kasuga, Kazuyuki,Hatakeyama, Hyoe,Hatakeyama, Tatsuko
, p. 1 - 14 (2007/10/02)
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.
