- SPIRO-LACTAM NMDA MODULATORS AND METHODS OF USING SAME
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 54; 56; 57
(2018/03/28)
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- SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 124
(2018/03/28)
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- Non-natural amino acids as modulating agents of the conformational space of model glycopeptides
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The synthesis and conformational analysis in aqueous solution of different α-methyl-α-amino acid di-amides, derived from serine, threonine, β-hydroxycyclobutane-α-amino acids, and their corresponding model β-O-glucopeptides, are reported. The study reveals that the presence of an α-methyl group forces the model peptides to adopt helix-like conformations. These folded conformations are especially significant for cyclobutane derivatives. Interestingly, this feature was also observed in the corresponding model glucopeptides, thus indicating that the α-methyl group and not the β-O-glucosylation process largely determines the conformational preference of the backbone in these structures. On the other hand, atypical conformations of the glycosidic linkage were experimentally determined. Therefore, when a methyl group was located at the Cβ atom with an R configuration, the glycosidic linkage was rather rigid. Never-theless, when the S configuration was displayed, a significant degree of flexibility was observed for the glycosidic linkage, thus showing both alternate and eclipsed conformations of the ψb dihedral angle. In addition, some derivatives exhibited an unusual value for the Φ2 angle, which was far from a value of -60° expected for a conventional β-O-glycosidic linkage. In this sense, the different conformations exhibited by these molecules could be a useful tool in obtaining systems with conformational preferences "a la carte".
- Fernandez-Tejada, Alberto,Corzana, Francisco,Busto, Jesus H.,Jimenez-Oses, Gonzalo,Peregrina, Jesus M.,Avenoza, Alberto
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supporting information; experimental part
p. 7042 - 7058
(2009/07/25)
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- PREPARATION, SPECTRAL AND PHYSICOCHEMICAL CHARACTERISTICS OF METHYLAMIDE Nα-PHENYLTHIOCARBAMOYL DERIVATIVES OF NATURALLY OCCURING AMINO ACIDS
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The methylamide Nα-phenylthiocarbamoyl derivatives of encoded amino acids II were prepared either by the addition of phenylisothiocyanate to amino acid methylamides or by the treatment of amino acid phenylthiohydantoins (5-alkyl-3-phenyl-2-thioxo-4-imidazolinones) I with methylamine.The derivatives were prepared of 19 amino acids and their melting points, 1H NMR, 13C NMR, mass, ultraviolet and infrared spectra were measured.
- Pavlik, Manfred,Kluh, Ivan,Pavlikova, Frantiska,Vasickova, Sona,Kostka, Vladimir
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p. 1940 - 1954
(2007/10/02)
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