52820-26-5

Upstream product

• 7719-09-7 thionyl chloride 
• 7400-08-0 para-coumaric acid 
• 123-08-0 4-hydroxy-benzaldehyde 

Downstream Products

• 66061-53-8 3-(4-hydroxy-phenyl)-1-naphtho[1,2-d]oxazol-2-yl-propenone 
• 72129-96-5 3,3'-bis-(4-hydroxy-phenyl)-1,1'-benzo[1,2-d;4,5-d']bisoxazole-2,6-diyl-bis-propenone 
• 356568-33-7 1-(4-Hydroxy-phenyl)-3-(2,4,6-trimethyl-phenyl)-propenone 
• 86293-51-8 1-(4-bromophenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one 
• 29838-16-2 3-(4-hydroxyphenyl)-1-(p-tolyl)prop-2-en-1-one 
• 66062-12-2 4-(4-hydroxy-phenyl)-6-naphtho[1,2-d]oxazol-2-yl-3-phenyl-3,4-dihydro-1H-pyrimidine-2-thione 
• 66061-65-2 4-(2-phenyl-5-naphtho[1,2-d]oxazol-2-yl-3,4-dihydro-2H-pyrazol-3-yl)-phenol 
• 66061-71-0 1-acetyl-5-(4-hydroxy-phenyl)-3-naphtho[1,2-d]oxazol-2-yl-4,5-dihydro-1H-pyrazole 
• 66062-11-1 4-(4-hydroxy-phenyl)-6-naphtho[1,2-d]oxazol-2-yl-3,4-dihydro-1H-pyrimidine-2-thione 
• 66061-59-4 4-(3-naphtho[1,2-d]oxazol-2-yl-4,5-dihydro-isoxazol-5-yl)-phenol 
• 72130-20-2 6,6'-bis-(4-hydroxy-phenyl)-1,1'-diphenyl-5,6,5',6'-tetrahydro-1H,1'H-4,4'-benzo[1,2-d;4,5-d']bisoxazole-2,6-diyl-bis-pyrimidine-2-thione 
• 72130-26-8 4,4'-(2,2'-diphenyl-3,4,3',4'-tetrahydro-2H,2'H-5,5'-benzo[1,2-d;4,5-d']bisoxazole-2,6-diyl-di-pyrazol-3-yl)-bis-phenol 
• 72130-14-4 6,6'-bis-(4-hydroxy-phenyl)-5,6,5',6'-tetrahydro-1H,1'H-4,4'-benzo[1,2-d;4,5-d']bisoxazole-2,6-diyl-bis-pyrimidine-2-thione 
• 72130-02-0 1,1'-diacetyl-5,5'-bis-(4-hydroxy-phenyl)-4,5,4',5'-tetrahydro-1H,1'H-3,3'-benzo[1,2-d;4,5-d']bisoxazole-2,6-diyl-bis-pyrazole 

Relevant academic research and scientific papers

Multifunctional novel Diallyl disulfide (DADS) derivatives with β-amyloid-reducing, cholinergic, antioxidant and metal chelating properties for the treatment of Alzheimer's disease

A series of novel Diallyl disulfide (DADS) derivatives were designed, synthesized and evaluated as chemical agents, which target and modulate multiple facets of Alzheimer's disease (AD). The results showed that the target compounds 5a-l and 7e-m exhibited significant anti-Aβ aggregation activity, considerable acetylcholinesterase (AChE) inhibition, high selectivity towards AChE over butyrylcholinesterase (BuChE), potential antioxidant and metal chelating activities. Specifically, compounds 7k and 7l exhibited highest potency towards self-induced Aβ aggregation (74% and 71.4%, 25 μM) and metal chelating ability. Furthermore, compounds 7k and 7l disaggregated Aβ fibrils generated by Cu2+-induced Aβ aggregation by 80.9% and 78.5%, later confirmed by transmission electron microscope (TEM) analysis. Besides, 7k and 7l had the strongest AChE inhibitory activity with IC50 values of 0.056 μM and 0.121 μM, respectively. Furthermore, molecular modelling studies showed that these compounds were capable of binding simultaneously to catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. All the target compounds displayed moderate to excellent antioxidant activity with ORAC-FL values in the range 0.546-5.86 Trolox equivalents. In addition, absorption, distribution, metabolism and excretion (ADME) profile and toxicity prediction (TOPKAT) of best compounds 7k and 7l revealed that they have drug like properties and possess very low toxic effects. Collectively, the results strongly support our assertion that these compounds could provide good templates for developing new multifunctional agents for AD treatment.

Design, synthesis and biological evaluation of novel carboline-cinnamic acid hybrids as multifunctional agents for treatment of Alzheimer's disease

Alzheimer's disease (AD) is a complex neurodegenerative disease with multiple pathological features. Multifunctional compounds able to simultaneously interact with several pathological components have been considered as a solution to treat the complex pathologies of neurodegenerative diseases. β-carboline and cinnamic acid have been extensively studied for their widespread biological effects in treatment of AD, further application is limited due to its poor solubility and high toxicity. Herein, a series of carboline-cinnamic acid hybrids was designed and synthesized to obtain new multifunctional molecules with low toxicity and good physicochemical properties. In particular, e3 and e12 exhibited significant inhibition of Aβ aggregation (inhibitory rate at 25 μM: 65% and 72% respectively), moderate BuChE inhibition, excellent neuroprotective effects and low neurotoxicity. Furthermore, in the AD mice model, e3 and e12 could restore learning and memory function to a comparable level to that of the control and did not exhibit any acute toxicity in vivo at a relatively high dose of 600 mg/kg. Thus, these new compounds can be further studied as multifunctional molecules for AD.

Coumarin derivative as well as preparation method and application thereof

The invention discloses a coumarin derivative as well as a preparation method and application thereof. The chemical structural formula of the coumarin derivative is represented by a formula (I) or a formula (II), wherein in the formula, R1 is H, CH3, OCH3

6-Cinnamoyl-4-arylaminothienopyrimidines as highly potent cytotoxic agents: Design, synthesis and structure-activity relationship studies

In this paper, we described the synthesis and cytotoxic activities of two new series of thieno[2,3-d]pyrimidine and thieno[3,2-d] pyrimidine derivatives. Most of the synthesized compounds had significant antiproliferative activities against PC3, MDA-MB-23

Coumarin glycoside compound, its preparation process and pharmaceutical composition and use thereof

The invention relates to a novel coumarin glycoside compound derived from esculine or skimmin and a synthesis method thereof, and application of the novel coumarin glycoside compound and 7-O-methylesculine as drugs in diseases related to diabetic angiopat

Phenylacrylate derivative and application thereof as neuroprotective drug

The invention discloses a phenylacrylate derivative and application thereof as a neuroprotective drug, the phenylacrylate derivative and a medicinal preparation thereof have a good curative treating effect on cranial nerve injury diseases such as cerebral apoplexy and related diseases, are low in acute toxicity and do not have the potential heart toxicity risk, and have a prominent technical effect and a substantial scientific progress compared with existing medicines. The phenylacrylate derivative is a compound represented by a general formula i or a salt thereof as shown in the specification.