1158-35-6

Usage

Uses

Used in Pharmaceutical Industry:
H-D-Lys(Z)-OMe . HCl is used as an intermediate in the synthesis of analgesic dipeptide derivatives for the treatment of pain. Its incorporation into these compounds enhances their analgesic properties, providing a potential alternative to conventional pain-relieving medications.
Used in Drug Development:
H-D-Lys(Z)-OMe . HCl is used as a building block in the development of novel pharmaceuticals with improved efficacy and reduced side effects. Its unique structure allows for the creation of innovative drug candidates that can target specific pain receptors or pathways, offering a more targeted approach to pain management.

Upstream product

• 67-56-1 methanol 
• 34404-32-5 (R)-2-amino-6-(((benzyloxy)carbonyl)amino)hexanoic acid 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 1437-00-9 Carbobenzoxy-D-valyl-ε-carbobenzoxy-D-lysin-methylester 
• 1437-02-1 Carbobenzoxy-D-valyl-ε-carbobenzoxy-L-lysin-methylester 
• 100103-10-4 Boc-Arg(NO₂)-D-Lys(Z)-OMe 
• 97485-07-9 N^α,N^ε-Bis(benzyloxycarbonyl)-D-lysyl-N^ε-(benzyloxycarbonyl)-D-lysine Methyl Ester 
• 328236-02-8 (R)-6-Benzyloxycarbonylamino-2-[(1-{4-[(3,5-dimethyl-phenylcarbamoyl)-methyl]-phenoxy}-cyclopentanecarbonyl)-amino]-hexanoic acid methyl ester 
• 100103-11-5 H-Arg(NO₂)-D-Lys(Z)-OMe*HCl 
• 100103-13-7 Boc-Tyr-Arg(NO₂)-D-Lys(Z)-OH 
• 100103-12-6 Boc-Tyr-Arg(NO₂)-D-Lys(Z)-OMe 
• 3949-03-9 Carbobenzoxy-D-valyl-ε-carbobenzoxy-D-lysin 
• 1436-72-2 Carbobenzoxy-L-valyl-ε-carbobenzoxy-D-lysin 

Relevant academic research and scientific papers

Unveiling the active isomer of cycloalanopine, a cyclic opine from: Lactobacillus rhamnosus LS8, through synthesis and analog production

Opines are widely distributed natural products formed by the reductive condensation of amino acids with α-keto acids or carbonyls of carbohydrates. They have important biological roles in bacteria, higher plants, fungi, invertebrates and mammals, including humans. An unusual cyclic opine of undefined stereochemistry, cycloalanopine, was previously isolated from Lactobacillus rhamnosus LS8 and reported to have antimicrobial activity against both Gram-negative and Gram-positive bacteria. In this work, we report a three-step strategy to synthetically access pure isomers of this cyclic compound and analogs thereof. In the key step, acyclic bis-hydrazides can be oxidized with (diacetoxyiodo) benzene to corresponding cyclic N,N-diacylhydrazides. The three cycloalanopine isomers, along with several analogs, were synthesized and tested against a panel of Gram-positive and Gram-negative bacteria. We identified the active isomer as the meso compound: (4R,6S)-4,6-dimethyl-1,2,5-triazepan-3,7-dione. Additionally, a glycine derivative, (R)-4-methyl-1,2,5-triazepan-3,7-dione, was ascertained to be more potent. This compound was active against both Gram-positive and Gram-negative organisms with the strongest potency against Escherichia coli and Acinetobacter baumannii, an opportunistic pathogen found in hospital-derived infections.

Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist

Analgesics with no abuse liability are highly demanded in the market. KOR agonists have been proved to be strong analgesics without MOR agonist-related side effects, such as respiratory depression, tolerance, and dependence liability; however, activation

PHENYL PROPANAMIDE DERIVATIVE, AND MANUFACTURING METHOD AND PHARMACEUTICAL APPLICATION THEREOF

The present invention provides a phenyl propanamide derivative as represented by formula (I), a manufacturing method of the derivative, application of the derivative as a κ-opioid receptor (KOR) agonist, and application of the derivative for manufacturing a pharmaceutical product for treating and/or preventing pain or a pain-related disease.

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.