- Asymmetric and Geometry-Selective α-Alkenylation of α-Amino Acids
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Both E- and Z-N′-alkenyl urea derivatives of imidazolidinones may be formed selectively from enantiopure α-amino acids. Generation of their enolate derivatives in the presence of K+ and [18]crown-6 induces intramolecular migration of the alkeny
- Abas, Hossay,Mas-Roselló, Josep,Amer, Mostafa Mahmoud,Durand, Derek J.,Groleau, Robin R.,Fey, Natalie,Clayden, Jonathan
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supporting information
p. 2418 - 2422
(2019/02/09)
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- UNNATURAL AMINO ACIDS
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The present invention relates to a process for the preparation compounds of Formula (I): Formula (I) wherein X, Z, Q, Ar, R1, R2, R3 and R4 are each as defined herein. The present invention also relates to processes for the preparation of the compounds of quaternary amino acids and hydantions, to compound of Formula(I), to intermediate compounds of Formula (II), to quaternary amino acid compounds of Formula (III) and to hydantoin compounds of Formula (IV).
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Paragraph 00182; 00196; 00199
(2018/07/05)
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- MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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- MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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- SUBSTITUTED IMIDAZOHETEROCYCLES
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The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
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Page/Page column 34; 35
(2009/01/24)
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- Squaric acid-based peptidic inhibitors of matrix metalloprotease-1
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A series of squaric acid-peptide conjugates were synthesized and evaluated as inhibitors of MMP-1. The cyclobut-3-enedione core was substituted at the 3-position with several functional groups, such as -N(alkyl)OH, -NHOH, and -OH, that are designed to bind to the zinc atom in the active site of the metalloprotease. The 4-position of the cyclobut-3-enedione was derivatized with mono- or dipeptides that are designed to bind in the S1′ and S2′ subsites of the enzyme, and position the metal chelating group appropriately in the active site for binding to zinc. Positional scanning revealed that -N(Me)OH provided the highest level of inhibition among the chelating groups that were tested, and Leu-Tle-NHMe was the preferred amino acid sequence. A combination of these groups yielded an inhibitor with an IC50 value of 95 μM. For one inhibitor, conversion of one of the carbonyl groups on the cyclobut-3-enedione core to a thiocarbonyl group resulted in a 18-fold increase in potency, and yielded a compound with an IC50 value of 15 μM.
- Onaran, M. Burak,Comeau, Anthony B.,Seto, Christopher T.
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p. 10792 - 10802
(2007/10/03)
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- Conformational Investigation of α,β-Dehydropeptides. II. Synthesis of Model Dipeptides
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Two series of models dipeptides: Ac-Pro-X-NHMe, where X = L-, D- and α,β-(Z)-Δ-Abu and L-, D- and α,β-(Z)-Δ-Leu, designed for conformational investigation of α,β-dehydroamino acid effect on peptide chain β-turn have been synthesized.
- Pietrzynski, Grzegorz,Rzeszotarska, Barbara
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- OXIDATIVE PREPARATION OF OPTICALLY ACTIVE N-HYDROXY-α-AMINO ACID AMIDES
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Two routes are presented for the conversion of optically active α-amino acid amides into the title compounds.One route (route A) features the formation of the Schiff's base 6 which is subsequently oxidized to the corresponding oxaziridines 7.Route B is ch
- Feenstra, R. W.,Stokkingreef, E. H. M.,Reichwein, A. M.,Lousberg, W. B. H.,Ottenheijm, H. C. J.,et al.
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p. 1745 - 1756
(2007/10/02)
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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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- Aqueous Solutions Containing Amino Acids and Peptides. Part 16. --Solute-Solute Interactions in Solutions Containing some N-Acetyl-N'-methylamino Acid Amides
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The energetics of the interactions occuring between some N-acetyl-N'-methylamino acid amides in aqueous solutions at 25 deg C have been investigated.Osmotic coefficients and enthalpies of dilution have been obtained for single-component and two-component
- Blackburn, G. Michael,Lilley, Terence H.,Milburn, Peter J.
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p. 2191 - 2206
(2007/10/02)
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