200059-78-5

Upstream product

• 331-39-5 caffeic acid 
• 107-05-1 3-chloroprop-1-ene 
• 200059-77-4 3-(3,4-bis-allyloxyphenyl)acrylic acid allyl ester 
• 106-95-6 allyl bromide 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 141-82-2 malonic acid 
• 71186-67-9 3,4-diallyloxybenzaldehyde 

Downstream Products

• 1190305-14-6 N-caffeoyl serotonin 
• 1383814-06-9 C₁₉H₂₀N₂O₄ 
• 200059-77-4 3-(3,4-bis-allyloxyphenyl)acrylic acid allyl ester 

Relevant academic research and scientific papers

Peramivir conjugates as orally available agents against influenza H275Y mutant

Peramivir is an efficacious neuraminidase (NA) inhibitor for treatment of influenza by intravenous administration. However, the efficacy of peramivir toward the H275Y mutant is appreciably reduced. To address this drawback, conjugation of peramivir with c

Kinsenoside derivatives with hypoglycemic activity and preparation method and application thereof

The invention belongs to the technical field of medicines, discloses structures of kinsenoside derivatives 1-6 and hypoglycemic activity of the kinsenoside derivatives 1-6, provides a preparation method of kinsenoside derivatives with remarkable hypoglycemic activity, and provides a technical scheme for developing a new VEGFR1 signal channel small-molecule inhibitor and finding a novel hypoglycemic approach. The kinsenoside derivatives provided by the invention can be used as a medicine for treating diabetes mellitus and a VEGFR1 inhibitor.

TRPV4 activity inhibitor

PROBLEM TO BE SOLVED: To provide a compound that inhibits TRPV4 activity and is useful for prevention or improvement of overactive bladder and irritable bowel syndrome or the like. SOLUTION: A TRPV4 activity inhibitor has a rosmarinic acid derivative selected from the formulae (Ia)-(Id) or a salt thereof as an active ingredient. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT

Phenethyl alcohol glucoside analogue and its synthetic method and application (by machine translation)

The invention discloses phenethyl alcohol glucoside analogue and its synthetic method and application. The invention uses biological electronic isostere of such drugs design principle obtain a series of a kind of transformation with neuroprotective activity of the phenethyl alcohol glucoside derivative, sialic acid methyl ester derivatives and 9 the methcoside [...] decarboxylative rosmarinic acid compounds. The invention further provides a method for synthesizing analogs of phenethyl alcohol glucoside. Nerve pharmacological experimental study found, the breeding invention benzene through like apoptotic, to anti-oxidative damage, increasing the cell survival, reduce the apoptosis rate, inhibiting the production of reactive oxygen species in cells, significantly reducing the damage of the cells, play a neuroprotective role. Phenethyl alcohol glucoside provided by the invention includes analogs in the prevention or treatment of neurodegenerative disease, cerebral ischemia, in neurological disorders has important application potential. (by machine translation)

Synthetic phenylethanoid glycoside derivatives as potent neuroprotective agents

Several phenylethanoid glycoside derivatives were designed and synthesized. Most of the synthetic compounds showed significant neuroprotective effects, including antioxidative and anti-apoptotic properties. Specifically, target compounds displayed potent effects against various toxicities such as H2O2 and 6-hydroxydopamine (6-OHDA) in PC12 cells. Among the synthetic derivatives, three compounds (5, 6, 8) exhibited much superior activities to the marketed drug Edaravone. The compounds were able to prevent the 6-OHDA-induced damage in PC12 cells in a dose-dependent manner. The anti-apoptotic effects could be observed via cell morphological changes. Moreover, the compounds significantly reduced the intracellular ROS increase resulting from 6-OHDA treatment. The preliminary structure-activity relationships were also explored. Compounds 5, 6, 8 may hold the potential as promising neuroprotective agents and new lead compounds for the treatment of neurodegenerative diseases or cerebral ischemia.

Synthesis and structure-activity relationships of serotonin derivatives effect on α-glucosidase inhibition

The α-glucosidase inhibitory activities of serotonin derivatives were evaluated. Two serotonin derivatives, N-p-coumaroyl serotonin (2) and N-caffeoyl serotonin (4) exhibited most potent inhibition on α-glucosidase, whereas, cinnamic acid derivatives were

Synthesis and structure-activity relationships of phenylpropanoid amides of serotonin on tyrosinase inhibition

In this manuscript, we synthesized a series of phenylpropanoid amide of serotonin 1-9, analyzed their structural importance for two biologic activities (antioxidant activity and tyrosinase inhibitory activity). While the serotonin moiety and the amide linkage of serotonin derivatives affect antioxidant activity strongly, the serotonin moiety, the amide linkage and the cinnamic acid moiety affect tyrosinase inhibitory activity. Among tested compounds, compound 4 which contains cathechol moiety exhibited the most antioxidant activity (EC50 = 19.4 ± 2.0 μM), and compound 6 exhibited significant tyrosinase inhibitory activity (IC50 = 5.4 ± 3.6 μM). Our data suggests that a useful clue for the design and development of new tyrosinase inhibitors.

Serotonin derivatives as inhibitors of β-secretase (BACE 1)

All serotonin derivatives described here (1-9) inhibited BACE 1 in a dose dependent manner. The 50% Inhibition Concentration (IC50) of N-cinnamoyl serotonin (1) was 86.7 ± 4.0 μM. The peptide conjugation of serotonin derivatives influenced the BACE 1 inhibitory activity. Among serotonin derivatives (1-8), introduction of substituents, such as hydroxyl and methoxy groups at the 4′-position decreased the inhibitory activity (N-p-coumaroyl serotonin (2), N-p-methoxy cinnamoyl serotonin (3)). With a hydroxylgroup at the 4′-position, and the meta-hydroxy function being substituted by a hydroxyl group or methoxy group (Ncaffeoyl serotonin (4), N-feruloyl serotonin (5)), inhibitory activity was weakened, (IC50 > 400 μM). BACE 1 inhibitory activity was effected by the substituents of the cinnamic acid moiety. This is the first report on Structure-Activity- Relationships (SAR) for the BACE 1-inhibiting activity of serotonin derivatives. These serotonin derivatives, which have anti-oxidative effects as well are expected to be useful in the study of the mechanisms of Alzheimer's disease.