40986-91-2

Upstream product

• 103-76-4 1-(2-hydroxyethyl)piperazine 
• 350-46-9 4-Fluoronitrobenzene 
• 100-02-7 4-nitro-phenol 
• 110-85-0 piperazine 
• 13288-06-7 1-(2-bromoethoxy)-4-nitrobenzene 

Downstream Products

• 255847-14-4 1-[(4-cyano-5-methyl-4-phenyl)hexyl]-4-[2-(4-aminophenoxy)ethyl]piperazine 
• 860032-26-4 8-hydroxy-5-[(R)-1-hydroxy-2-(2-{4-[4-(2-piperazin-1-yl-ethoxy)-phenylamino]-phenyl}-ethylamino)-ethyl]-1H-quinolin-2-one 
• 1008423-34-4 8-benzyloxy-5-[(R)-1-(tert-butyl-dimethyl-silanyloxy)-2-(2-{4-[4-(2-piperazin-1-yl-ethoxy)-phenylamino]-phenyl}-ethylamino)-ethyl]-1H-quinolin-2-one 
• 946689-19-6 C₁₂H₁₉N₃O 
• 910378-69-7 N-[4-[2-[4-[(3,4-dihydro-6-methoxy-2,2,7,8-tetramethyl-2H-1-benzopyran-5-yl)methyl]piperazin-1-yl]ethoxy]phenyl]methanesulfonamide 
• 910378-64-2 4-{2-[4-[(3,4-dihydro-6-methoxy-2,2,7,8-tetramethyl-2H-1-benzopyran-5-yl)methyl]piperazin-1-yl]ethoxy}aniline 
• 910378-59-5 1-[(3,4-dihydro-6-methoxy-2,2,7,8-tetramethyl-2H-1-benzopyran-5-yl)methyl]-4-[2-(4-nitrophenoxy)ethyl]piperazine 
• 255846-82-3 1-[(4-cyano-5-methyl-4-phenyl)hexyl]-4-[2-(4-nitrophenoxy)ethyl]piperazine 

Relevant academic research and scientific papers

Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques

The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.

Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof

The invention discloses diphenoxyl flexible molecules with high affinity with A[beta] plaque and a preparation method and applications thereof. After the molecules are labeled by radionuclide, the molecules can be used as an A[beta] plaque developing agen

Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD

A multivalent approach focused on amine-based secondary binding groups was applied to the discovery of long-acting inhaled β2-agonists. Addition of amine moieties to the neutral secondary binding group of an existing β2-agonist serie

Synthesis and biological evaluation of benzopyran analogues bearing class III antiarrhythmic pharmacophores

We have synthesized a series of compounds combining the hydroxy-benzopyran ring of vitamin E with the methylsulfonylaminophenyl group of class III antiarrhythmic drugs, connected through tertiary amine moieties. Evaluation of the antiarrhythmic and antioxidant activity of the new compounds was carried out on isolated rat heart preparations using the non-recirculating Langendorff mode. The new analogues were present, at 10 μM concentration, during ischemia and reperfusion. Selected compounds were further studied by a conventional microelectrode method in order to get insight into their cellular mode of action. The most active compound, N-[4-[2-[[2-(3,4-dihydro-6-hydroxy-2,2,7,8-tetramethyl-2H-1-benzopyran-5 -yl)ethyl] methylamine]ethyl]phenyl]methanesulfonamide (19a), reduces premature beats, prolongs QT and QRS intervals during ischemia and reperfusion, and reduces MDA content, leading to a fast recovery of the heart. In addition, it exhibits moderate class III antiarrhythmic action.

Discovery of novel neuronal voltage-dependent calcium channel blockers based on emopamil left hand as a bioactive template

A series of novel neuronal voltage-dependent calcium channel (VDCC) blockers, with inhibitory activity at low micromolar and moderate solubility in water, was discovered by constructing and screening a focused library based on emopamil (1) left hand (ELH)

Piperidinyl and piperazinyl derivatives

Compounds of the formula: STR1 in which R1 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO2,--CN, 1-imidazolyl or 1,2,4-triazol-1-yl; Y is STR2 --CH2 --, --O--, --S--, or --SO2 --; X is --CH= or --N=; R2 is hydrogen when n is 0, otherwise it is hydrogen or --OH; n is one of the integers 0, 1, 2, 3, 4, 5 or 6; A is STR3 where R3 is alkylsulfonamido of 1 to 6 carbons atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl; or STR4 where R4 is hydrogen or alkyl of 1 to 6 carbon atoms; with the provisos that; a) X is --CH= when Y is STR5 --O-- or --S-- and when Y is STR6 and R2 is --OH; b) X is --N= when A is STR7 c) A is STR8 when Y is --S-- or --SO2 -- and X is --CH=, and their pharmaceutically acceptable salts are Class III antiarrhythmic agents.