55456-40-1

Usage

Uses

Used in Pharmaceutical Research:
H-Aib-OBzl is used as a building block in peptide synthesis for its unique structure and stability, which aids in the development of new drugs and therapies.
Used in Medicinal Chemistry:
H-Aib-OBzl is utilized as a component in the design and synthesis of novel compounds with potential medicinal properties, leveraging its ability to mimic natural amino acids.
Used in Drug Development:
H-Aib-OBzl is employed in the creation of new pharmaceutical agents, contributing to advancements in drug discovery and therapeutic innovation.

Upstream product

• 62-57-7 2-Aminoisobutyric acid 
• 100-51-6 benzyl alcohol 
• 84758-57-6 tert-butoxycarbonylamino-2-methyl-propionic acid benzyl ester 
• 60421-20-7 benzyl 2-amino-2-methylpropionate hydrochloride 
• 100-44-7 benzyl chloride 

Downstream Products

• 124180-77-4 N,N-Adipoyl-bis-(α-amino-isobutyryl-α-amino-isobuttersaeure-benzylester) 
• 84758-57-6 tert-butoxycarbonylamino-2-methyl-propionic acid benzyl ester 
• 79118-35-7 Boc-L-Pro-Aib-OBzl 
• 79118-36-8 Boc-MeA-MeA-OBzl 
• 84758-63-4 Z-L-Ala-Aib-OBzl 
• 79118-31-3 Boc-Gln-Aib-OBzl 
• 124125-86-6 Boc-MeA(d6)-MeA-OBzl 
• 79118-16-4 α-Aminoisobutyric acid benzyl ester p-toluenesulfonate 
• 79118-23-3 Boc-Leu-Aib-OBzl 
• 203636-24-2 Fmoc-Val-Aib-OBn 
• 211372-14-4 Fmoc-Aib-Aib-OBzl 
• 254112-92-0 2-[2-(3-benzyl-3-tert-butoxycarbonylamino-2-oxo-azetidin-1-yl)-acetylamino]-2-methyl-propionic acid benzyl ester 
• 98477-29-3 Boc-Phe-Aib-OBzl 
• 401518-84-1 benzyl 2-{4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]piperidin-1-yl}-2-methylpropanoate 

Relevant academic research and scientific papers

N-Pyrrolidine-based α/β-peptides incorporating ABOC, a constrained bicyclic β-amino acid, for asymmetric aldol reaction catalysis

A series of N-pyrrolidine-based α,β-peptide catalysts incorporating a constrained 2-aminobicyclo[2.2.2]octane carboxylic acid (ABOC) residue were synthesized and evaluated in the asymmetric aldol reaction from acetone and some p-substituted benzaldehydes. Their catalytic properties were shown to be highly dependent on the amino acid sequences and on the absolute configuration of the ABOC residue that played a determinant role. Among the peptides tested, the heterochiral tripeptide H-Pro-(R)-ABOC-Asp-OCH3 13, that adopts a turn conformation in the solid state, proved to be the most efficient catalyst affording β-hydroxy ketones in high yields and good enantioselectivities (up to 87%).

Synthesis, preferred conformation, and membrane activity of medium-length peptaibiotics: Tylopeptin B

The solid-phase synthesis and full chemical characterization of the medium-length (14-amino acid residues) peptaibol with antibiotic properties of tylopeptin B, originally extracted from the fruiting body of the mushroom Tylopilus neofelleus, are described. These data are accompanied by the results on the solution-phase synthesis via the segment condensation approach of a selected, side-chain protected, analog. A solution conformational analysis, performed by the combined use of FTIR absorption, circular dichroism, and 2D-NMR (the latter technique coupled to molecular dynamics calculations), favors the conclusion that the 3D-structure of tylopeptin B is largely helical with a preference for the α- or the 310-helix type depending upon the nature of the solvent. Helix topology and (partial) amphiphilic character are responsible for the observed membrane-modifying properties of this peptaibiotic.

Cyclopropanecarboxylic acid esters as potential prodrugs with enhanced hydrolytic stability

Esters of cyclopropanecarboxylic acid demonstrate a substantial increase in stability under both acid- and base-catalyzed hydrolytic conditions. Comparison of the stability of valacyclovir 13 with the cyclopropane analogue 14 shows that at 40 °C and pH 6 the half-life of 14 is >300 h while the value for 13 is 69.7 h. CBS-QB3 calculations on isodesmic reactions for transfer of groups from an alkane to an ester show that a cyclopropyl group provides hyperconjugative stabilization.

PHOSPHORAMIDATE PRODRUGS FOR TREATMENT OF VIRAL INFECTION

The invention concerns 2'-methyl ribonucleotide phosphoramidates which are neutral prodrugs which are converted in vivo to 2'- methyl ribonucleotide triphosphates. These compounds are useful in the treatment of viral infection. Of particular interest are prodrugs of a methylsulfonylhydrazinyl purine 2'-methyl nucleotide triphosphate: 2'methyl- N6-alkyl-N6- (N-methylsulfonamide) adenosine triphosphate and its 2-amino derivative.

PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF

The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc. ; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

Lipopeptaibol metabolites of tolypocladium geodes: Total synthesis, preferred conformation, and membrane activity

We have synthesized by solution methods and characterized the lipopeptaibol metabolite LP237-F8 extracted from the fungus Tolypocladium geodes and five selected analogues with the Etn → Aib or Etn → Nva replacement at position 8 and/or a triple Gln → Glu(OMe) replacement at positions 5, 6, and 9 (Etn = Cα-ethylnorvaline, Aib = α-aminoisobutyric acid, Nva = norvaline). Conformation analysis, performed by FT-IR absorption, NMR, and CD techniques, strongly supports the view that the six terminally blocked decapeptides are highly helical in solution. Helix topology and amphiphilic character are responsible for their remarkable membrane activity. At position 8 the combination of high hydrophobicity and Ca tetrasubstitution, as in the Etn-containing LP237-F8 metabolite, has a positive effect on membrane interaction.

Carboxyalkylureido cephalosporins

Carboxyalkylureido cephalosporins of the formula STR1 wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group STR2 R1 is hydrogen or methoxy; A is strai

N-chloro-amino acid derivatives activity

There is provided, a novel class of compounds exhibiting antibacterial activity, said compounds having the formula: EQU1 wherein X and Y each represent a member which may be the same or different selected from the group consisting of H and Cl with the pri