DISUBSTITUTED BETA-LACTONES AS INHIBITORS OF N-ACYLETHANOLAMINE ACID AMIDASE (NAAA)
The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.
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Paragraph 0369; 0370
(2013/06/06)
Modular solid-phase synthesis of teroxazoles as a class of α-helix mimetics
α-Helices are ubiquitous structural elements of proteins and are important in molecular recognition. Small molecules mimicking α-helices have proven to be valuable biophysical probes or modulators of protein-protein interactions. Here, we present modeling studies and the modular solid-phase synthesis of teroxazole derivatives as a new class of α-helix mimetics. The synthesis is compatible with a variety of functional groups and should thus be generally applicable for generating diversely substituted oligo-oxazole scaffolds. The teroxazole scaffold is predicted to be polar and to project peptidomimetic side chains at positions i, i+3, and i+6 of an α-helix, which complements projection patterns of existing helix mimetics. The scaffold retains sufficient conformational flexibility to conform to induced-fit models of protein-protein interaction inhibition. Copyright
Pinto Gomes, Cristiano,Metz, Alexander,Bats, Jan W.,Gohlke, Holger,Goebel, Michael W.
supporting information; experimental part
p. 3270 - 3277
(2012/07/02)
Oprical resolution of β-Hydroxynorvaline
β-Hydroxy-DL-norvaline (HyNva) was successfully separated into its diastereoisomers by fractional crystallization from 2-propanol as p-toluenesulfonic acid (TsOH) salts.The two racemic diastereoisomers were resolved into four stereoisomers by Vogler's method, using diastereisomers of the N-benzyloxycarbonyl DL-amino acid and L-tyrosine hydrazide.
Yamada, Masaki,Okawa, Kenji
p. 2889 - 2890
(2007/10/02)
Synthesis of aliphatic 2-amino-3-hydroxy acids and separation of their diastereoisomers with the aid of copper chelates.
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MIX
p. 41 - 48
(2007/10/06)
Synthetic alpha-amino-beta-hydroxyvaleric acids.
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BUSTON,CHURCHMAN,BISHOP
p. 665 - 668
(2007/10/12)
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