cas 19036-43-2, 3-AMINO-2,2-DIMETHYL-PROPANOIC ACID

Articles about 19036-43-2Total 11 be found

Thermodynamic Scale of β-Amino Acid Residue Propensities for an α-Helix-like Conformation
A thiol-thioester exchange system has been used to measure the propensities of diverse β-amino acid residues to participate in an α-helix-like conformation. These measurements depend on formation of a parallel coiled-coil tertiary structure when two peptide segments become linked by thioester formation. One peptide segment contains a "guest" site that accommodates diverse β residues and is distal to the coiled-coil interface. We find that helix propensity is influenced by side chain placement within the β residue [β3 (side chain adjacent to nitrogen) slightly favored relative to β2 (side chain adjacent to carbonyl)]. The previously recognized helix stabilization resulting from five-membered ring incorporation is quantified. These results are significant because so few quantitative thermodynamic measurements have been reported for α/β-peptide folding.
Fisher, Brian F.,Hong, Seong Ho,Gellman, Samuel H.
p. 9396 - 9399
(2018/08/07)

Palladium(0)/PAr3-catalyzed intermolecular amination of C(sp3)-H bonds: Synthesis of β-amino acids
An intermolecular C(sp3)-H amination using a Pd0/PAr3 catalyst was developed. The reaction begins with oxidative addition of R2N-OBz to a Pd0/PAr3 catalyst and subsequent cleavage of a C(sp3)-H bond by the generated Pd-NR2 intermediate. The catalytic cycle proceeds without the need for external oxidants in a similar manner to the extensively studied palladium(0)-catalyzed C-H arylation reactions. The electron-deficient triarylphosphine ligand is crucial for this C(sp3)-H amination reaction to occur.
He, Jian,Shigenari, Toshihiko,Yu, Jin-Quan
p. 6545 - 6549
(2015/06/08)

NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
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(2015/08/04)

NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
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(2015/05/06)

4 -HYDROXY- ISOQUINOLINE COMPOUNDS AS HIF HYDROXYLASE INHIBITORS
The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
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(2013/09/26)

METHOD FOR THE PREPARATION OF OMEGA-AMINO-ALKANEAMIDES AND OMEGA-AMINO-ALKANETHIOAMIDES AS WELL AS INTERMEDIATES OF THIS METHOD
The present invention relates to method for the preparation of an ω-amino-alkane(thio)amide having the formula (3). Furthermore, novel intermediates and partial reaction steps of the claimed method are disclosed.
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(2012/02/05)

Approaches for the synthesis of functionalized cryptophycins
The first syntheses of bioactive cryptophycins functionalized at unit D were accomplished in a one-pot Staudinger reduction/cyclization step. An azido precursor for the lower part of the backbone was introduced to minimize protective group chemistry and enable a very convenient synthesis of cryptophycin-52 and unit D cryptophycin analogues containing an ester or a free carboxylic acid for bioconjugations. Both new cryptophycin derivatives show high biological activity in cytotoxicity assays.
Sammet, Benedikt,Bogner, Tobias,Nahrwold, Markus,Weiss, Christine,Sewald, Norbert
experimental part
p. 6953 - 6960
(2010/12/18)

One-pot synthesis of β-amino acid derivatives via addition of bis(O-silyl) ketene acetals on iminium salts
We report here our findings on a new and highly efficient strategy for the synthesis of β-amino acids involving the addition of bis(O-silyl) ketene acetals on Mannich type iminium electrophiles.
Moumné, Roba,Denise, Bernard,Parlier, Andrée,Lavielle, Solange,Rudler, Henri,Karoyan, Philippe
p. 8277 - 8280
(2008/03/30)

Synthesis of 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives and evaluation of their affinity for MHC class-II proteins
1,2,5-Thiadiazolidin-3-one 1,1-dioxide derivatives (±)-1a-d and (±)-2 were designed by molecular modeling as MHC (major histocompatibility complex) class-II inhibitors. They were prepared from the unsymmetrically N,N'- disubstituted acyclic sulfamides (±)
Ducry, Laurent,Reinelt, Stefan,Seiler, Paul,Diederich, Francois,Bolin, David R.,Campbell, Robert M.,Olson, Gary L.
p. 2432 - 2447
(2007/10/03)

Primary Aminomethylation at the α-Position of Carboxylic Acids and Esters. Trimethylsilyl Triflate-Catalyzed Reaction of Ketene Silyl Acetals with N,N-Bis(trimethylsilyl)methoxymethylamine
A new, general method for the synthesis of β-aminocarboxylic esters (9) and acids (10) was developed.The introduction of primary aminomethyl unit at the α-position of carboxylic esters (2) and acids (3) was achieved in high yields by the silyl trifluorome
Okano, Kohji,Morimoto, Toshiaki,Sekiya, Minoru
p. 2228 - 2234
(2007/10/02)