120926-60-5

Upstream product

• 54244-69-8 tert-butoxycarbonylamino-acetic acid benzyl ester 
• 76-05-1 trifluoroacetic acid 
• 100-39-0 benzyl bromide 
• 77930-08-6 C₁₉H₂₁F₂N₂O₅P 
• 1738-68-7 Gly-OBz 

Downstream Products

• 204640-68-6 (E)-4-{2-[(E)-Benzyloxycarbonylmethylimino-methyl]-phenoxy}-but-2-enoic acid ethyl ester 
• 130676-99-2 benzyl (3-bromopropionamido)acetate 
• 102115-73-1 N-chloroacetylglycine benzyl ester 
• 1203698-05-8 Boc-Arg(Mtr)-Gly-OBn 

Relevant academic research and scientific papers

A minimalistic approach to identify substrate binding features in B1 Metallo-β-lactamases

The 2-oxoazetidinylacetate sodium salt was synthesized as a model of a minimal β-lactam drug. This compound and the monobactam aztreonam were assayed as substrates of the Metallo-β-lactamase BcII. None of them was hydrolyzed by the enzyme. While the azeti

Synthesis of poly(ester-amide) dendrimers based on 2,2-Bis(hydroxymethyl) propanoic acid and glycine

Water-soluble, biodegradable, and biocompatible poly(ester-amide) dendrimers with hydroxyl functional groups are synthesized from previously prepared AB2 adduct of 2,2-bis(hydroxymethyl) propanoic acid (bis-MPA) and glycine as a repeating unit. Two esterification procedures using different coupling reagent/catalyst systems (DCC/DPTS or EDC/DMAP) are studied with respect to efficiency, ease of products purification, and quality of the final products. Both procedures have their own benefits and drawbacks, depending on dendrimer generation. The synthesized poly(ester-amide) dendrimers as well as commercially available bis-MPA dendrimers, poly(ester-amide) hyperbranched polymer, and poly(vinyl alcohol) are used for preparation of solid dispersions of sulfonylurea antidiabetic drug glimepiride to improve its poor water-solubility. In vitro dissolution studies show in comparison with pure glimepiride in crystalline or amorphous form, to the same extent improved glimepiride solubility for solid dispersions based on dendritic polymers, but not for poly(vinyl alcohol). The amount of glimepiride complexed with both dendrimer types increases with dendrimer generation.

DRUGS TO TREAT OCULAR DISORDERS

The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

PEG-BASED DENDRON AND PROCESS FOR PRODUCING THE SAME

It is provided a process for preparing biodegradable dendrons based on poly(ethyleneglycol) (PEG), as well as novel biodegradable dendrons based on PEG. The present invention also provides conjugates of the biodegradable dendrons of the present invention with biomolecules and conjugates for use as medicaments.

NOVEL COMPOUNDS

A compound of formula (I) or a pharmaceutically acceptable derivative thereof, (formula 1) wherein R1,R2, R3, R4, R5, X, m and n are defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.

Cyclic RGD peptidomimetics containing bifunctional diketopiperazine scaffolds as new potent integrin ligands

The synthesis of eight bifunctional diketopiperazine (DKP) scaffolds is described; these were formally derived from 2,3-diaminopropionic acid and aspartic acid (DKP-1-DKP-7) or glutamic acid (DKP-8) and feature an amine and a carboxylic acid functional group. The scaffolds differ in the configuration at the two stereocenters and the substitution at the diketopiperazinic nitrogen atoms. The bifunctional diketopiperazines were introduced into eight cyclic peptidomimetics containing the Arg-Gly-Asp (RGD) sequence. The resulting RGD peptidomimetics were screened for their ability to inhibit biotinylated vitronectin binding to the purified integrins αvβ 3 and αvβ5, which are involved in tumor angiogenesis. Nanomolar IC50 values were obtained for the RGD peptidomimetics derived from trans DKP scaffolds (DKP-2-DKP-8). Conformational studies of the cyclic RGD peptidomimetics by 1H NMR spectroscopy experiments (VT-NMR and NOESY spectroscopy) in aqueous solution and Monte Carlo/Stochastic Dynamics (MC/SD) simulations revealed that the highest affinity ligands display well-defined preferred conformations featuring intramolecular hydrogen-bonded turn motifs and an extended arrangement of the RGD sequence [Cβ(Arg)-Cβ(Asp) average distance ≥8.8 A]. Docking studies were performed, starting from the representative conformations obtained from the MC/SD simulations and taking as a reference model the crystal structure of the extracellular segment of integrin αvβ3 complexed with the cyclic pentapeptide, Cilengitide. The highest affinity ligands produced top-ranked poses conserving all the important interactions of the X-ray complex. Copyright

ETUDE D'UN SCHEMA DE SYNTHESE PEPTIDIQUE INTRAMOLECULAIRE A L'AIDE DE DERIVES DU PHOSPHORE TETRAEDRIQUE

A new scheme of repetitive and controlled peptide synthesis offers two advantages compared to the usual methods of synthesis: two steps only are used for the prolongation of a peptide chain with an amino-acid residue and the risk of racemisation is minimized.The two postulated steps are verified particularly by the rearrangement, in an alkaline alcoholic medium, of phosphordiamides 1 incorporating one amino-acid residue, leading to the formation of the peptide derivatives 6 and 8.The severe limitations of this method are discussed.