150652-96-3Relevant articles and documents
Efficient synthesis of novel glutamate homologues and investigation of their affinity and selectivity profile at ionotropic glutamate receptors
Pinto, Andrea,Tamborini, Lucia,Mastronardi, Federica,Ettari, Roberta,Romano, Diego,Nielsen, Birgitte,De Micheli, Carlo,Conti, Paola
supporting information, p. 1980 - 1982 (2014/04/17)
A convenient synthesis of four new enantiomerically pure acidic amino acids is reported and their affinity at ionotropic glutamate receptors was determined. The new compounds are higher homologues of glutamic acid in which the molecular complexity has bee
Exploring Leishmania major Inositol Phosphorylceramide Synthase (LmjIPCS): Insights into the ceramide binding domain
Mina, John G.,Mosely, Jackie A.,Ali, Hayder Z.,Denny, Paul W.,Steel, Patrick G.
supporting information; experimental part, p. 1823 - 1830 (2011/04/26)
The synthesis of set of ceramide analogues exploring hydrophobicity in the acyl chains and the degree and nature of hydroxylation is described. These have been assayed against the parasitic protozoan enzyme LmjIPCS. These studies showed that whilst the C-3 hydroxyl group was not essential for turnover it provided enhanced affinity. Reflecting the membrane bound nature of the enzyme a long (C13) hydrocarbon ceramide tail was necessary for both high affinity and turnover. Whilst the N-acyl chain also contributed to affinity, analogues lacking the amide linkage functioned as competitive inhibitors in both enzyme and cell-based assays. A model that accounts for this observation is proposed.
SPIRO (PIPERIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRIFLUOROMETHYL PHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS
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Page/Page column 86, (2009/12/05)
Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C 1-4 alkyl; R1 is hydrogen, C 1-4 alkyl, C(O)OH, C(O)NH2 or (C 1-4 alkylene)R10; R2 and R3 are independently hydrogen, C 1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C 1-4 alkyl, C 1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C 1-4 alkylene) R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C 1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C 1-4 alkyl), C(O)N(C 1-4 alkyl)2 or C(O)OH; n is O, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.