85607-73-4

Upstream product

• 160893-68-5 m-methoxycarbonylphenyl propargyl ether 
• 19438-10-9 methyl 3-hydroxybenzoate 
• 99-06-9 3-Carboxyphenol 
• 106-96-7 propargyl bromide 
• 91920-00-2 ethyl 3-(prop-2-yn-1-yloxy)benzoate 

Downstream Products

• 936125-18-7 tert-butyl 2-(3-(prop-2-ynyloxy)benzamido)ethylcarbamate 
• 946570-04-3 3-prop-2-ynyloxy-benzoic acid 2,5-dioxopyrrolidin-1-yl ester 
• 936125-22-3 tert-butyl 2,2',2''-(10-(2-oxo-2-(3-(prop-2-ynyloxy)benzamido)ethylamino)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetate 
• 1207193-10-9 S-2,4,6-trimethoxybenzyl 3-(prop-2-ynyloxy)benzothioate 
• 1292783-94-8 C₆₅H₈₁N₁₃O₁₆S₂ 
• 909185-76-8 C₂₀H₁₄O₆ 
• 1450817-83-0 C₂₁H₁₆O₆ 

Relevant academic research and scientific papers

Metal-Free Catalyzed Cyclization of N-Methoxybenzamides to Construct Quaternary Carbon-Containing Isoindolinones

Through the intramolecular cyclization of N-methoxybenzamides, a simple and efficient method for constructing valuable isoindolinones under metal-free conditions was developed. The reaction was featured by employing low-cost catalyst, simple operation, 100% atomic economy and excellent regioselectivity. Moreover, a detailed computational study on the reaction system has been performed to clarify the mechanism. This protocol tolerated a variety of functional groups and provided a metal-free protocol for the synthesis of chromane- or tetrahydroquinoline-fused isoindolinones in good yields.

BIFUNCTION CHEMICAL EPIGENENTIC MODIFIERS AND METHODS OF USE

The present disclosure relates to bifunctional chemical epigenetic modifiers, and methods of making, kits and using the bifunctional chemical epigenetic modifiers. The bifunctional chemical epigenetic modifiers can include a FK506 molecule or derivative thereof, a linker and a bifunctional ligand. The bifunctional ligand can be a histone deacetylase inhibitor.

1, 2, 4 - Oxadiazole Nrf2 activator - tacrine split product as well as preparation method and application thereof

The invention discloses 1,oxadiazole Nrf2 activator - tacrine split products as well as a preparation method and application thereof. The invention relates to an acetylcholinesterase inhibitory activity. Nrf2 Activation activity, selective screening and Morris water maze test was carried out to evaluate the compound of general formula I, II, III for the treatment of's disease (in particular, severe's disease), found to have good in vitro, in vivo activity and extremely high selectivity, and can be used as a precursor substance for further development through selective inhibition of acetylcholinesterase and activation Nrf2.

Donepezil-oxadiazole fusion compound and preparation method and application thereof

The invention discloses a donepezil-oxadiazole fusion compound, the structural formula of which is shown in formula (I), (II) (III) or (IV). The invention also discloses a preparation method of the donepezil-oxadiazole fusion compound and application of the donepezil-oxadiazole fusion compound in preparation of drugs for treating Alzheimer's disease. The donepezil-oxadiazole fusion compound has novel structure, has various activities such as inhibitor cholinesterase, Nrf2 pathway activation and the like, can improve acetylcholine level in the brain and activate antioxidant stress reaction of cells.

Natural-Product-Inspired Aminoepoxybenzoquinones Kill Members of the Gram-Negative Pathogen Salmonella by Attenuating Cellular Stress Response

Gram-negative bacteria represent a challenging task for antibacterial drug discovery owing to their impermeable cell membrane and restricted uptake of small molecules. We herein describe the synthesis of natural-product-derived epoxycyclohexenones and explore their antibiotic activity against several pathogenic bacteria. A compound with activity against Salmonella Typhimurium was identified, and the target enzymes were unraveled by quantitative chemical proteomics. Importantly, two protein hits were linked to bacterial stress response, and corresponding assays revealed an elevated susceptibility to reactive oxygen species upon compound treatment. The consolidated inhibition of these targets provides a rationale for antibacterial activity and highlights epoxycyclohexenones as natural product scaffolds with suitable properties for killing Gram-negative Salmonella.

One-pot esterification-click (CuAAC) and esterification-acetylene coupling (Glaser/Eglinton) for functionalization of Wang polystyrene resin

We report three new sets of one-pot reactions for functionalization of Wang polystyrene resin and its derivatives. We first show that it is possible to combine esterification and CuAAC (Copper-Catalyzed Alkyne-Azide Cycloaddition) in a one-pot reaction wi

COUPLING OF POLYPEPTIDES AT THE C-TERMINUS

The present invention relates to novel polypeptides, methods for their synthesis, pharmaceutical compositions comprising the novel polypeptides as well as their use in medicaments for therapeutic applications.

Synthesis of DOTA-conjugated multivalent cyclic-RGD peptide dendrimers via 1,3-dipolar cycloaddition and their biological evaluation: Implications for tumor targeting and tumor imaging purposes

This report describes the design and synthesis of a series of αVβ3 integrin-directed monomeric, dimeric and tetrameric cyclo[Arg-Gly-Asp-d-Phe-Lys] dendrimers using "click chemistry". It was found that the unprotected N-ε-azido derivative of cyclo[Arg-Gly-Asp-d-Phe-Lys] underwent a highly chemoselective conjugation to amino acid-based dendrimers bearing terminal alkynes using a microwave-assisted Cu(i)-catalyzed 1,3-dipolar cycloaddition. The αVβ 3 binding characteristics of the dendrimers were determined in vitro and their in vivo αVβ3 targeting properties were assessed in nude mice with subcutaneously growing human SK-RC-52 tumors. The multivalent RGD-dendrimers were found to have enhanced affinity toward the αVβ3 integrin receptor as compared to the monomeric derivative as determined in an in vitro binding assay. In case of the DOTA-conjugated 111In-labeled RGD-dendrimers, it was found that the radiolabeled multimeric dendrimers showed specifically enhanced uptake in αVβ3 integrin expressing tumors in vivo. These studies showed that the tetrameric RGD-dendrimer had better tumor targeting properties than its dimeric and monomeric congeners. This journal is The Royal Society of Chemistry.