65160-62-5

Upstream product

• 4530-20-5 BOC-glycine 
• 1080-06-4 L-Tyr-OMe 
• 34805-17-9 methyl 2S-amino-3-(4-benzyloxyphenyl)propionate hydrochloride 
• 3417-91-2 L-tyrosine methyl ester HCl 

Downstream Products

• 119463-06-8 (tert-butoxycarbonyl)glycyl-L-tyrosine 
• 1196734-96-9 (S)-methyl 2-(2-((tert-butoxycarbonyl)amino)acetamido)-3-(3,4-dihydroxyphenyl)propanoate 
• 5845-66-9 3-(S)-(4-hydroxy-benzyl)-piperazine-2,5-dione 
• 96935-86-3 H-Gly-Tyr-OMe 
• 717139-76-9 (S)-2-[2-(5-Fluoro-2,4-dinitro-phenylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionic acid methyl ester 
• 3885-05-0 N-t-butyloxycarbonyl-glycyl-L-tyrosine-hydrazide 

Relevant academic research and scientific papers

Histamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation

Alzheime?s disease (AD) is the most prominent neurodegenerative disorder with high medical need. Protein-protein-interactions (PPI) interactions have a critical role in AD where β-amyloid structures (Aβ) build toxic oligomers. Design of disease modifying multi target directed ligand (MTDL) has been performed, which disable PPI on the one hand and on the other hand, act as procognitive antagonists at the histamine H3 receptor (H3R). The synthetized compounds are structurally based on peptidomimetic amino acid-like structures mainly as keto, diketo-, or acyl variations of a piperazine moiety connected to an H3R pharmacophore. Most of them showed low nanomolar affinities at H3R and some with promising affinity to Aβ-monomers. The structure–activity relationships (SAR) described offer new possibilities for MTDL with an optimized profile combining symptomatic and potential causal therapeutic approaches in AD.

Application of High-Throughput Competition Experiments in the Development of Aspartate-Directed Site-Selective Modification of Tyrosine Residues in Peptides

Herein we report a Cu-catalyzed, site-selective functionalization of peptides that employs an aspartic acid (Asp) as a native directing motif, which directs the site of O-arylation at a proximal tyrosine (Tyr) residue. Through a series of competition studies conducted in high-throughput reaction arrays, effective conditions were identified that gave high selectivity for the proximal Tyr in Asp-directed Tyr modification. Good levels of site-selectivity were achieved in the O-arylation at a proximal Tyr residue in a number of cases, including a peptide-small molecule hybrid.

Cyclizing pentapeptides: Mechanism and application of dehydrophenylalanine as a traceless turn-inducer

Dehydrophenylalanine is used as a traceless turn-inducer in the total synthesis of dichotomin E. Macrocyclization of the monomer is achieved in high yields and selectivity over cyclodimerization under conditions 100 times more concentrated than previously achieved. The enamide facilitates ring closing, and Rh-catalyzed hydrogenation of the unsaturated cyclic peptide results in selective formation of the natural product or its epimer, depending on our choice of phosphine ligand. NMR analysis and molecular modeling revealed that the linear peptide adopts a left-handed α-turn that preorganizes the N- and C-termini toward macrocyclization.

Synthesis and biological evaluation of analogue of delavayin-C: A cyclic heptapeptide

The synthesis of N-methylated analogue of delavayin-C, a cyclic heptapeptide was carried out by using solution phase technique. The structure of this compound was confirmed on the basis of analytical IR, 1H NMR and FAB MASS spectral data. The e

Water-soluble tripeptide Aβ (9-11) forms amyloid-like fibrils and exhibits neurotoxicity

(Chemical Equation Presented) A water-soluble, hydrophilic tripeptide GYE, having sequence identity with the N-terminal segment of amyloid peptides Aβ(9-11), upon self-association exhibits amyloid-like fibrils and significant neurotoxicity towards the Neu

Synthesis of a novel 14-membered highly constrained cyclic peptidic scaffold

The synthesis and NMR analysis of a novel highly constrained scaffold is described. The 14-membered macrocyclic ring structure was inspired by many medicinally relevant natural products that also contain the bi-aryl ether moiety. The synthesis required on

Sequential Tyrosyl Polypeptides: Part I - Synthesis and IR Studies

Alternating sequential tyrosyl polypeptides, (XY)n (where X is glycine, L-alanine or L-valine, and Y is L-tyrosine) have been synthesized by polymerizing azide or N-hydroxysuccinimide ester of the respective dipeptides.The conformation of the p