138111-12-3

Upstream product

• 6515-05-5 2',4'-bis(methoxymethoxy)acetophenone 
• 100-10-7 4-dimethylamino-benzaldehyde 
• 89-84-9 2',4'-dihydroxy-4-acetophenone 
• 121-69-7 N,N-dimethyl-aniline 
• 65490-08-6 2-hydroxy-4-(methoxymethoxy)acetophenone 

Downstream Products

• 1250377-77-5 C₂₄H₂₃FN₄O₃ 
• 637753-80-1 6-hydroxy-4'-dimethylaminoaurone 

Relevant academic research and scientific papers

Antioxidant and Cardioprotective Evaluation of Some N-(3-Chloro-2-oxo-4-arylazetidin-1-yl)-2-[(4-oxo-2-aryl-4H-chromen-7-yl)oxy]acetamide Derivatives

A series of N-(3-chloro-2-oxo-4-arylazetidin-1-yl)-2-[(4-oxo-2-aryl-4H-chromen-7-yl)oxy]acetamide derivatives [SLP VI 1(a-d)-2(a-d)] were synthesized from 7-hydroxy flavone derivatives through the intermediate Schiff bases. The synthesized compounds were investigated for in vitro antioxidant property by DPPH radical scavenging assay. The title compounds with good antioxidant potency were further evaluated for possible cardioprotective effect by doxorubicin induced cardiotoxicity. All biochemical changes were normalized after oral administration of the test compounds at the dose of 50 μg/kg. The results showed the significant (p 0.05) increase in antioxidant enzymes catalase and superoxide dismutase in heart tissue homogenates. These observations enable us to conclude that the synthesized derivatives SLP VI 1b, VI 1c, VI 2b and VI 2d have cardioprotective activity against doxorubicin induced cardiotoxicity. Further, an attempt has been made to perform in silico studies on the synthesized compounds to predict the interaction between test ligands and prospective cardiovascular protein targets using molecular docking tools. The title compounds have good binding affinity with MAPkinase P38 and PKCβ cardiovascular targets.

Synthesis and biological evaluation of isoliquiritigenin derivatives as a neuroprotective agent against glutamate mediated neurotoxicity in HT22 cells

Glutamate-induced neurotoxicity is characterized by cellular Ca2+ uptake, which is upstream of reactive oxygen species (ROS)-induced apoptosis signaling and MAPKs activation. In the present study, we synthesized isoliquiritigenin analogs with electron-donating and electron-withdrawing functional groups. These analogs were evaluated for neuroprotective effect against glutamate-induced neurotoxicity in HT22 cells. Among these analogs, compound BS11 was selected as a potent neuroprotective agent. Cellular Ca2+ concentration, ROS level, MAPKs activation and AIF translocation to the nucleus were increased upon treatment with 5 mM glutamate. In contrast, we identified that compound BS11 reduced the cellular Ca2+ concentration and ROS level upon glutamate exposure. Western blot analysis showed that MAPK activation was decreased by treatment with compound BS11. We further identified that cotreatment of compound BS11 and glutamate inhibited translocation of AIF to the nucleus.

Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells

Bone diseases may not be imminently life-threatening or a leading cause of death such as heart diseases or cancers. However, as aging population grows in almost every part of the world, they surely impose significant socioeconomic burden on the society, not to mention the patients and their families. Osteoporosis is the most common type of bone disease, which frequently develops in seniors, especially in postmenopausal women. Although currently several anti-osteoclastic drugs designed to suppress excessive osteoclast activation, a major cause of osteoporosis, are commercially available, accompanying adverse effects ranging from mild to severe have been reported as well. Natural products have become increasingly popular because of their effectiveness with fewer side effects. Isoliquiritigenin (ILG), a natural flavonoid from licorice, has been reported to suppress osteoclast differentiation and activation. In the present study, newly synthesized ILG derivatives were screened for their anti-osteoporotic activity as more potent substitute candidates to ILG. Out of the 12 ILG derivatives tested, two compounds demonstrated significantly improved bone loss in vitro by inhibiting both osteoclastogenesis and osteoclast activity. The results of the present study indicate that these compounds may serve as a potential drug for osteoporosis and warrant further studies to evaluate their in vivo efficacy.

In vitro and in vivo anticancer studies of 2′-hydroxy chalcone derivatives exhibit apoptosis in colon cancer cells by hdac inhibition and cell cycle arrest

Considering the therapeutic values of bioflavonoids in colon cancer treatment, six 2′-hydroxy chalcones (C1-C6) were synthesized, characterized and screened for in vitro cytotoxicity on human colon carcinoma (HCT116) and African green monkey kidney epithe

Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease

A series of 4'-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50= 4.91 μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic analysis of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Aβ1-42aggregation and Cu2+-induced Aβ1-42aggregation by 89.5% and 79.7% at 25 μM respectively, as well as acted as a selective monoamine oxidase B inhibitor (IC50= 0.29 μM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer's disease.

A kind of compounds with analgesic effect and its preparation method (by machine translation)

This invention relates to a kind of compounds with analgesic effect and its preparation method, the structural formula of this compound as the following I, II, III or IV is shown, wherein R is the chemical formula is C n H 2n+1 straight chain alkyl, n=1-7. The invention also discloses the above-mentioned several kinds of different structural formula of compound preparation method, the preparation of the same and the application of the capsaicin receptor inhibitors. The present invention provides the compound has strong analgesic activity, more than du Lengding part, and pharmacological experiment has not found this compound has addiction side effects. The present invention provides the compound plus pharmaceutically acceptable vector can be prepared as pharmaceutical compositions and pharmaceutical preparation, and can be developed with the addiction of preparing a medicine analgesia class. (by machine translation)

Calcium hydroxide is an efficient catalyst for synthesis of polyhydroxy chalcones

Calcium hydroxide was found to be an efficient catalyst for synthesis of polyhydroxy chalcones. This method has been employed to synthesize various 2′,4′-dihydroxychalcones having various substituents on the B ring. The merits of this method include shorter reaction time, inexpensive and easily available catalyst, high yield, and easy workup compared to other reported methods. Copyright Taylor and Francis Group, LLC.

Synthesis, docking studies and antioxidant activity of some chalcone and aurone derivatives

Chalcones and aurones are found to possess high antioxidant activity. They are known to inhibit tyrosinase enzyme involved in synthesis of melanin. A series of substituted chalcones and aurones have been synthesized and tested for their antioxidant activi

Synthesis and pharmacological screening of some novel chalconyl derivatives of substituted phenyl semicarbazide

In the present study, we have synthesized chalcone and semicarbazide-linked chalonyl derivatives and the titled compounds confirmed by MS, IR, and 1H NMR techniques. The anticonvulsant activity was determined by maximal electroshock (MES) induced seizure method. A majority of the compounds exhibited significant anticonvulsant activity after intraperitoneal administration. The results show the importance of hydrogen bonding for activity. In the present study 5e, 5h, 5i, 6e, 6h, and 6i emerged as the most active molecules, showed significant anticonvulsant of activity. Springer Science+Business Media, LLC 2010.

Chalconsemicarbazone: A new scaffold for antiepileptic drug discovery

During our investigation in the area of epileptic drug discovery, we have identified that the available conventional antiepileptic drugs are effective in 60-80% patients and in specific type of seizures and having various undesirable side effects. But in present time a new class aryl semicarbazone is emerged as new pharmacophore in epileptic drug discovery having broad spectrum activity. On the bases of work done in this area we have applied hybridization of pharmacophore strategy of drug design and developed a new pharmacophore. We have also designed a scheme for synthesizing such pharmacophore and performed their pharmacological screening for the protection of seizures, behavioral study and CNS activity. The compound 1-[1-(2,4-dihydroxyphenyl)-3-(2-hydroxyphenyl) allylidene]-4-(2-fluorophenyl) semicarbazide (8) emerged as the most active prototype molecule in all the models.