13515-95-2

Upstream product

• 67-56-1 methanol 
• 56-87-1 L-lysine 
• 657-27-2 L-Lysine hydrochloride 
• 77-76-9 2,2-dimethoxy-propane 
• 75-77-4 chloro-trimethyl-silane 
• 70-53-1 2,6-diaminohexanoic acid hydrochloride 
• 26124-78-7 (S)-α-lysine hydrochloride 
• 13734-28-6 Boc-Lys-OH 
• 17929-90-7 3-aminoazepan-2-one 

Downstream Products

• 943590-99-6 C₂₃H₂₉N₃O₅ 
• 1373445-42-1 methyl 6-amino-2-[2-(2,3-dimethylphenylamino)benzamido]hexanoate 
• 1404074-26-5 N-((4-(-2-benzoyl-3-methylguanidino)butyl)-1-methyl-5-oxoimidazolidin-2-ylidene)benzamide 
• 98048-25-0 Trt-Lys(Trt)-OMe 
• 24498-31-5 (S)-methyl 2-amino-6-(benzyloxycarbonylamino)hexanoate 
• 106086-18-4 Methyl N,N'-α,ε-bis(N-tert-butyloxycarbonyl-2-phenylthiazolidine-4-carbonyl)-L-lysine 
• 62056-78-4 C₃₁H₃₄N₂O₄P₂ 
• 21568-87-6 2-aminocaprolactam 
• 170455-81-9 N,N-di(N-benzyloxy-N-acetyl-β-alanyl)lysine methyl ester 
• 2483-48-9 (+)-(S)-N₂,N₆-bis[(1,1-dimethylethoxy)carbonyl]-lysine methyl ester 
• 897932-10-4 N,O-bis(3,4-dimethoxycarbonylcaffeoyl)-L-lysine methyl ester 
• 897932-09-1 (S)-2,6-Bis-(3,4,5-tris-methoxycarbonyloxy-benzoylamino)-hexanoic acid methyl ester 

Relevant academic research and scientific papers

Synthesis, characterization and topical application of novel bifunctional peptide metallodendrimer

Present research work focuses on the synthesis of lower generation bifunctional peptide metallodendrimer followed by its characterization using IR, Mass and NMR (1H and 13C) and finally exploring it for treating acne and wounds. Metallodendrimer was formulated into Tamarind Seed Polysaccharide (TSP) based hydrogel at 7% w/w concentration and analyzed for its properties of spreadability and bioadhesion. Testing of in-vitro antibacterial activity, sterility, in-vivo wound healing efficacy and stability studies followed the formulation development stage. The explored peptide metallodendrimer is a complex of second generation lysine dendrimers and zinc, exhibiting antibacterial activity against Propionibacterium acne, Staphylococcus epidermidis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. In-vivo wound healing studies in comparison with marketed product indicated significant performance by metallodendrimer with respect to percent re-epithelization and wound contracture. The results were supported by concurrent improvement in various histopathological parameters such as cellularity, granulation, epithelization, vascular density, collagen staining intensity with less number of average mast cells and absence of scar formation. A bifunctional peptide metallodendrimer based platform technology was fabricated and duly evaluated for potential activities.

Understanding the binding properties of phosphorylated glycoluril-derived molecular tweezers and selective nanomolar binding of natural polyamines in aqueous solution

A modular synthetic platform for the construction of flexible glycoluril-derived molecular tweezers was developed. The binding properties of four exemplary supramolecular hosts obtained via this approach towards 16 organic amines were investigated by means of 1H NMR titration. In this work, we compare the Ka values obtained this way with those of three structurally related molecular tweezers and provide a computational approach towards an explanation of the observed behavior of those novel hosts. The results showcase that certain structural modifications lead to very potent and selective binders of natural polyamines, with observed binding of spermine below 10 nM. This journal is

NOVEL DRUG DELIVERY CONJUGATED MOIETY FOR ORAL ADMINISTRATION OF DRUG UNSUITABLE FOR ORAL ADMINISTRATION AND PREPARATION METHOD THEREOF

The present invention provides a novel drug delivery conjugated moiety for oral administration of a drug that is not suitable for oral administration or a pharmaceutically acceptable salt thereof. When the drug delivery conjugated moiety of the present invention or a pharmaceutically acceptable salt thereof is combined with a drug, which is not suitable for oral administration, and is administered orally, it exhibits an excellent absorption rate without decreasing the biological activities of the drug. Moreover, the drug delivery conjugated moiety of the present invention or a pharmaceutically acceptable salt thereof can be easily prepared in a few steps, which is very advantageous in terms of mass production.

Supramolecular self-assembly of chiral polyimides driven by repeat units and end groups

Pyromellitic diimides (PMDIs) are effective building blocks for the construction of supramolecular systems but are infrequently used in comparison with other electron-deficient aromatic systems. We report PMDI-based chiral polyimides that form polymeric supramolecular systems with unique self-assembly features that show time-dependent spectroscopic behaviour. Extensive investigations revealed the driving forces for the self-assembly of the polyimides. One is the complementary aromatic π-π stacking between electron-accepting PMDI and electron-donating phenyl ring in the polymer backbones, and another is the hydrogen bonding interactions of the end groups. The self-assembly is readily disrupted by guest molecules with strong associations with the PMDI and the end groups. The introduction of flexible arylether diimides into the PMDI-based copolymer backbones and the sequence of PMDIs and arylether diimides in the copolymer backbones significantly influence the self-assembly of the polyimides. The results elucidate the mechanisms of polymeric self-assembly of chiral polyimides, providing important information for the development of materials based on polymeric supramolecular systems with properties and functions regulated by composition, sequence and end groups.

Novel chiral derivatizing agents for 1H NMR determination of enantiomeric purities of carboxylic acids

(S)-4-(3-Aminopyrrolidin-1-yl)coumarin (1), (S)-4-(3-aminopiperidin-1-yl)coumarin (4), and (S)-4-(3-aminoazepan-1-yl)coumarin (7), prepared from 4-chlorocoumarin and (S)-pyrrolidin-3-amine, (S)-piperidin-3-amine, and (S)-azepan-3-amine, respectively, were proven to be versatile and reliable 1H NMR optical purity determination agents for chiral carboxylic acids.

AMINO ACID DERIVATIVES AND ABSORBABLE POLYMERS THEREFROM

The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.

Radical arylation of tyrosine residues in peptides

The radical arylation of the phenolic side chain of tyrosine in peptides was investigated. Aryl radicals were generated from aryldiazonium salts using titanium(III) chloride as stoichiometric reductant. Due to the high selectivity with which 3-aryltyrosine derivatives were formed, this reaction type represents a new strategy for the direct functionalization of peptides.

Novel aminopeptidase N inhibitors with improved antitumor activities

A series of aminopeptidase N (APN) inhibitors were designed and synthesized. Enzyme inhibitory, docking and antiproliferative studies were performed to evaluate the derived molecules. Molecule D15, with IC50 values of 10.9 μM, showed the best performance in the APN enzymatic inhibition assay. The binding pattern of molecule D9 and D15 in the active site of APN was predicted by docking studies. Hydrophobic and H-bond interactions were discovered to make key roles in the ligand-receptor bindings. Compared with the previous C7, several molecules such as D9, D14 and D15, exhibited significantly improved activities in inhibiting the growth of HL-60, ES-2, A549 and PLC cell lines.

A simple synthesis of 6-hydroxynorleucine based on the rearrangement of an N-nitrosodichloroacetamide

6-Hydroxynorleucine is a versatile chemical intermediate that has found broad use in target-oriented syntheses of numerous biologically active molecules. Despite its widespread use, and despite the various strategies that have been reported for its prepar

Synthesis and properties of bis-porphyrin molecular tweezers: Effects of spacer flexibility on binding and supramolecular chirogenesis

Ditopic binding of various dinitrogen compounds to three bisporphyrin molecular tweezers with spacers of varying conformational rigidity, incorporating the planar enediyne (1), the helical stiff stilbene (2), or the semi-rigid glycoluril motif fused to the porphyrins (3), are compared. Binding constants Ka = 104-106 M-1 reveal subtle differences between these tweezers, that are discussed in terms of porphyrin dislocation modes. Exciton coupled circular dichroism (ECCD) of complexes with chiral dinitrogen guests provides experimental evidence for the conformational properties of the tweezers. The results are further supported and rationalized by conformational analysis.