26787-75-7Relevant academic research and scientific papers
Semi-Rigid Nitroxide Spin Label for Long-Range EPR Distance Measurements of Lipid Bilayer Embedded β-Peptides
Wegner, Janine,Valora, Gabriele,Halbmair, Karin,Kehl, Annemarie,Worbs, Brigitte,Bennati, Marina,Diederichsen, Ulf
, p. 2203 - 2207 (2019)
β-Peptides are an interesting new class of transmembrane model peptides based on their conformationally stable and well-defined secondary structures. Herein, we present the synthesis of the paramagnetic β-amino acid β3-hTOPP (4-(3,3,5,5-tetramethyl-2,6-dioxo-4-oxylpiperazin-1-yl)-d-β3-homophenylglycine) that enables investigations of β-peptides by EPR spectroscopy. This amino acid adds to the, to date, sparse number of β-peptide spin labels. Its performance was evaluated by investigating the helical turn of a 314-helical transmembrane model β-peptide. Nanometer distances between two incorporated β3-hTOPP labels in different environments were measured by using pulsed electron/electron double resonance (PELDOR/DEER) spectroscopy. Due to the semi-rigid conformational design, the label delivers reliable distances and sharp (one-peak) distance distributions even in the lipid bilayer. The results indicate that the investigated β-peptide folds into a 3.2514 helix and maintains this conformation in the lipid bilayer.
Cp?Co(III)/MPAA-Catalyzed Enantioselective Amidation of Ferrocenes Directed by Thioamides under Mild Conditions
Liu, Yan-Hua,Li, Peng-Xiang,Yao, Qi-Jun,Zhang, Zhuo-Zhuo,Huang, Dan-Ying,Le, Minh Dong,Song, Hong,Liu, Lei,Shi, Bing-Feng
supporting information, (2019/03/19)
Cp?Cobalt(III)-catalyzed enantioselective C-H amidation of ferrocenes using monoprotected amino acids (MPAAs) as chiral ligands was developed. The reaction was performed under mild conditions in high yields (up to 97%) with moderate enantioselectivity (up to 77.5:22.5 er), providing a promising strategy to create planar chirality via base-metal-catalyzed enantioselective C-H activation.
BENZOTHIAZEPINE AND BENZOTHIADIAZEPINE DERIVATIVES WITH ILEAL BILE ACID TRANSPORT (IBAT) INHIBITORY ACTIVITY FOR THE TREATMENT HYPERLIPIDAEMIA
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Paragraph 0198, (2018/01/13)
The present invention relates to compounds of formula (I) wherein Rv, R1, R2, Rx, Ry, M, Rz, v, R3, R4, R5 and R6 are as defined within; pharmace
D - P-hydroxy-glycine derivatives and their preparation method and application
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Paragraph 0097; 0098, (2017/08/26)
The invention discloses a D-hydroxy phenylglycine derivative. Please see the formula of the D-hydroxy phenylglycine derivative in the specification. D-hydroxy phenylglycine serves as a parent body, amino groups and carboxyl groups of the D-hydroxy phenylglycine are reasonably modified, a phenolic hydroxyl group is connected with an aromatic nucleus type hydrophobic group through a connector, the D-hydroxy phenylglycine derivative which is novel in structure is constructed, compounds capable of promoting the secreting activity of GLP-1 and/or inhibiting the activity of Nav1.7 are screened out, the preparation method of the compounds is simple and can be used for preparing GLP-1secernent and/or Nav1.7 inhibitors, and the D-hydroxy phenylglycine derivative has potential application prospects in the fields of diabetes treatment drugs and/or neuropathy pain treatment drugs. Please see the formula in the specification.
Relaxing substrate specificity in antibody-catalyzed reactions: Enantioselective hydrolysis of N-Cbz-amino acid esters
Tanaka, Fujie,Kinoshita, Keiko,Tanimura, Ryuji,Fujii, Ikuo
, p. 2332 - 2339 (2007/10/03)
For a catalytic antibody to be generally useful for organic synthetic chemistry, it must be able to accept a broad range of substrates, yet retain high selectivity. In this work, we propose a hapten design to endow antibody catalysts with two opposing qualities, such as high enantioselectivity and broad substrate specificity. Racemic hapten 2 induced two separate classes of catalytic antibodies to hydrolyze either the L- or D-isomers of N-Cbz-amino acid esters 1. In the kinetic resolution of racemic ester 9, antibodies 7G12 and 3G2 gave 96% ee of L-10 and 94% ee of D-10, respectively. In addition, antibody 7G12 displayed broad substrate specificity, hydrolyzing the L-esters of Ala (1a), Leu (1b), Norleu (1c), Met (1d), Phe (1e), Val (1f), and phenylglycine (1g) with high enantioselectivity. Antibody 3G2 also hydrolyzed the D-isomers of these esters without sacrificing the enantioselectivity. This observation suggests that the use of haptens that fit snugly into the antigen-combining site, and leave the linker moiety outside, is an effective approach for the generation of catalytic antibodies with high selectivity and broad substrate applicability.
An Approach to a Synthetic Carboxylate-binding Pocket Based on β-Avoparcin
Stone, Martin J.,Dyk, Martha S. van,Booth, Paul M.,Williams, Dudley H.
, p. 1629 - 1635 (2007/10/02)
An approach to a macrocyclic lactam designed to bind to a carboxylate anion is described.The diaryl ether 8 was synthesised by Ullmann coupling of the protected 3-hydroxyphenylglycine derivative 7 and (E)-4-bromocinnamic acid methyl ester.Elaboration of an optically pure (R)-tyrosine synthon was achieved by transfer of electrophilic azide to the N-acyl oxazolidinone 12.The synthesis of a model system is also described.
