154591-14-7Relevant academic research and scientific papers
NORVALINE DERIVATIVE AND METHOD FOR PREPARATION THEREOF
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Page/Page column 28; 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.
