Category: 61343-99-5

Kim, Doyeon published the artcileIdentification and characterization of potent, selective and metabolically stable IKKβ inhibitor, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is rhodanine derivative preparation IKKbeta inhibitor structure activity; Allosteric inhibitor; IKKβ inhibitor; NF-κB; Reumatoid arthritis.

The authors have previously reported the identification of a rhodanine compound (I) with well-balanced inhibitory activity against IKKβ and collagen-induced TNFα activated cells. However, the authors need more optimized compounds because of its instability over plasma and microsome. As part of a program directed toward the optimization of IKKβ inhibitor, the authors modified a substituent of parent compound to a series of functional groups. Among substituted compounds, fluorine substituent (II) on the para position of Ph ring restored the stability toward plasma and microsome while retaining inhibitory potency and selectivity against IKKβ over other kinases. Also, the authors have demonstrated that compound (II) is an ATP non-competitive inhibitor and safe enough to apply to animal experiment from an acute toxicity test.

Bioorganic & Medicinal Chemistry Letters published new progress about Acute toxicity. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kumar, Praveen published the artcileAnticonvulsant and neurotoxicity evaluation of some novel 3-{[substituted]-amino}-2-phenyl-3H-quinazolin-4-one, Application of 4-(4-Chlorophenoxy)benzaldehyde, the main research area is anticonvulsant neurotoxicity aminophenylquinazolinone preparation structure activity.

Various 3-{[substituted]-amino}-2-phenyl-3H-quinazolin-4-one were synthesized and screened for anticonvulsant activity in maximal electroshock induced seizure (MES) and s.c. metrazol (scMET) induced seizure models in mice. The neurotoxicity was assessed using the Rotorod method. The 3-{[4-(4-Fluoro-phenoxy)-benzylidene]-amino}-2-phenyl-3H-quinazolin-4-one 7b and 3-{[4-(4-Chloro-3-methyl-phenoxy)-benzylidene]-amino}-2-phenyl-3H-quinazolin-4-one 7e emerged as the most promising compounds with anti-MES activity in mice i.p. All the compounds exhibited no neurotoxicity in Rotorod method.

International Journal of Pharmacology and Biological Sciences published new progress about Anticonvulsants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application of 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tripathi, Laxmi published the artcileAnticonvulsant and neurotoxicity evaluation of some novel cyclohexyl-[4-substituted benzylidene/2-oxo-1,2-dihydro-indol-3-ylidene]thiosemicarbazides, Application In Synthesis of 61343-99-5, the main research area is cyclohexyl amine reaction carbon sulfide hydrazine; thiosemicarbazide cyclohexyl preparation condensation aryl aldehyde; isatin condensation cyclohexyl thiosemicarbazide; arylidene thiosemicarbazide preparation anticonvulsant neurotoxicity activity; indolonylidene thiosemicarbazide preparation anticonvulsant neurotoxicity activity; thiosemicarbazone preparation anticonvulsant neurotoxicity activity.

A series of novel cyclohexyl-[4-substituted benzylidene/2-oxo-1,2-dihydro-indol-3-ylidene]thiosemicarbazides were synthesized and screened for anticonvulsant activity in maximal electroshock induced seizure (MES) and s.c. metrazol (scMET) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. The compounds cyclohexyl-[4-(4-chlorophenoxy)-benzylidene]thiosemicarbazide and cyclohexyl-[2-oxo-1,2-dihydro-indol-3-ylidene]thiosemicarbazide emerged as the most promising one with anti-MES activity in mice i.p. All the compounds exhibited no neurotoxicity in rotorod method.

Asian Journal of Chemistry published new progress about Anticonvulsants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application In Synthesis of 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tripathi, Laxmi published the artcileDesign, synthesis and anticonvulsant evaluation of novel N-(4-substituted phenyl)-2-[4-(substituted) benzylidene]-hydrazinecarbothio amides, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is phenyl benzylidene hydrazinecarbothioamide preparation; epilepsy anticonvulsant neurotoxicity structure activity docking pharmacokinetic study.

Thirty six new N-(4-substituted phenyl)-2-[4-(substituted) benzylidene]-hydrazinecarbothioamides were synthesized and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity was established in three seizure models i.e. MES, scMET and 6 Hz model. The most active compound was 2-[4-(4-chlorophenoxy)benzylidene]-N-(4-fluorophenyl)hydrazinecarbothioamide, I, which showed 100% protection at 0.5 h in the 6 Hz test. Compound 2-[4-(4-bromophenoxy) benzylidene]-N-(4-bromophenyl) hydrazinecarbothioamide, II, was found to be active in both the MES and 6 Hz test. A computational study was carried out from calculation of a pharmacophore pattern and the prediction of pharmacokinetic properties. Titled compounds have also exhibited good binding properties with epilepsy mol. targets such as glutamate, GABA (A) delta and GABA (A) alpha-1 receptors, in the Lamarckian genetic algorithm based on flexible docking studies.

European Journal of Medicinal Chemistry published new progress about Anticonvulsants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kumar, Praveen published the artcileComputational Study and Synthesis of a New Class of Anticonvulsants with 6 Hz Psychomotor Seizure Test Activity: 2-(1,3-benzodioxol-5-yloxy)- N′-[substituted]-acetohydrazides, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is anticonvulsant drug psychomotor seizure test; 2-(1; 3-benzodioxol-5-yloxy)-N’-[substituted]-acetohydrazides; 6 Hz psychomotor seizure test; computational study; docking; neurotoxicity.; synthesis.

About 50 million epileptic cases worldwide and 12 million in India are reported. Currently, available drugs yield adequate control of seizure in 60-70% of patients and show many toxic effects. These actualities provoked the search for novel, more efficacious and safer anticonvulsants. The concatenation of 2-(1,3-benzodioxol-5-yloxy)-N′-[substituted]-acetohydrazides SA 1- 10 was designed by mol. hybridization, optimized by computational study and synthesized with the objective of obtaining a prototype of potent anticonvulsant mols. especially active against partial seizures. Computational study was performed to calculate the pharmacophoric design, projection of the pharmacokinetic parameters and docking scores of the titled compounds with mol. targets of epilepsy. The anticonvulsant activity was ascertained by 6 Hz psychomotor seizure test. Minimal motor impairment showing neurotoxicity was assessed using the Rotarod test. Titled compounds possessed the indispensable elements of pharmacophore and displayed good binding affinity with mol. targets of epilepsy, such as GABA (A) alpha-1 & delta receptor, glutamate receptor, Na+/H+ exchanger and GABA- aminotransferase in docking studies. The most potent compound of the concatenation was 2-(1,3-benzodioxol-5-yloxy)-N′-[4-(4- chlorophenoxy)benzylidene]-acetohydrazide SA 4, showing 100% protection at four different time points with ED50 value 146.8 mg/kg at a TPE of 1 h in mice. The protection shown in 6 Hz test is implicated as the compound′s ability to control partial seizures. Thus, the titled compounds can be considered as potential prototype candidates for antiepileptic therapy against partial seizures.

Medicinal Chemistry (Sharjah, United Arab Emirates) published new progress about Anticonvulsants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tripathi, Laxmi published the artcileDesign & synthesis of N’-[substituted] pyridine-4-carbohydrazides as potential anticonvulsant agents, SDS of cas: 61343-99-5, the main research area is pyridine carbohydrazide derivative preparation anticonvulsant activity neurotoxicity; pharmacophore pharmacokinetic docking pyridinecarbohydrazide.

A series of N’-[substituted] pyridine-4-carbohydrazides were designed and synthesized keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity of the titled compounds was established after i.p. administration in three seizure models, which include MES, scMET and 6 Hz model. The most active compound of the series was N’-[4-(4-fluorophenoxy)benzylidene]pyridine-4-carbohydrazide (I), which showed a MES ED50 value of 128.3 mg/kg and 6 Hz ED50 value of 53.3 mg/kg in mice. The median toxic dose (TD50) was 343.6 mg/kg, providing compound I with a protection index of 2.67 in the MES test and 6.44 in 6 Hz test. A computational study was also carried out, including calculation of pharmacophore pattern, prediction of pharmacokinetic properties and docking studies.

European Journal of Medicinal Chemistry published new progress about Anticonvulsants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, SDS of cas: 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ashraf-Uz-Zaman, Md. published the artcileDesign, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer, COA of Formula: C13H9ClO2, the main research area is structure preparation urea compound FGFR1 inhibitor metastatic breast cancer; Blood-brain-barrier; FGFR1; In silico; Neurotoxicity; Synthesis; Triple-negative breast cancer.

Triple-neg. breast cancer (TNBC) is an aggressive type of cancer characterized by higher metastatic and reoccurrence rates, where approx. one-third of TNBC patients suffer from the metastasis in the brain. At the same time, TNBC shows good responses to chemotherapy, a feature that fuels the search for novel compounds with therapeutic potential in this area. Recently, we have identified novel urea-based compounds with cytotoxicity against selected cell lines and with the ability to cross the blood-brain barrier in vivo. We have synthesized and analyzed a library of more than 40 compounds to elucidate the key features responsible for the observed activity. We have also identified FGFR1 as a mol. target that is affected by the presence of these compounds, confirming our data using in silico model. Overall, we envision that these compounds can be further developed for the potential treatment of metastatic breast cancer.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, COA of Formula: C13H9ClO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Hobson, Adrian D. published the artcileDiscovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders, Application of 4-(4-Chlorophenoxy)benzaldehyde, the main research area is sphingosine phosphate receptor agonist neurodegenerative disorder.

S1P5 is one of 5 receptors for sphingosine-1-phosphate and is highly expressed on endothelial cells within the blood-brain barrier, where it maintains barrier integrity in in vitro models. Little more is known about the effects of S1P5 modulation due to the absence of tool mols. with suitable selectivity and drug-like properties. We recently reported that mol. A-971432 (Harris, 2010) (29 in this paper) is highly efficacious in reversing lipid accumulation and age-related cognitive decline in rats. Herein we describe the development of a series of selective S1P5 agonists that led to the identification of compound 29, which is highly selective for S1P5 and has excellent plasma and CNS exposure after oral dosing in preclin. species. To further support its suitability for in vivo studies of S1P5 biol., we extensively characterized 29, including confirmation of its selectivity in pharmacodynamic assays of S1P1 and S1P3 function in rats. In addition, we found that 29 improves blood-brain barrier integrity in an in vitro model and reverses age-related cognitive decline in mice. These results suggest that S1P5 agonism is an innovative approach with potential benefit in neurodegenerative disorders involving lipid imbalance and/or compromised blood-brain barrier such as Alzheimer’s disease or multiple sclerosis.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application of 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Bittel, Amy M. published the artcileVaried Length Stokes Shift BODIPY-Based Fluorophores for Multicolor Microscopy, SDS of cas: 61343-99-5, the main research area is boron dipyrromethene aromatic aldehyde fluorophore stokes shift multicolor microscopy.

Multicolor microscopy tools necessary to localize and visualize the complexity of subcellular systems are limited by current fluorophore technol. While com. fluorophores cover spectral space from the UV to the near IR region and are optimized for conventional bandpass based fluorescence microscopy, they are not ideal for highly multiplexed fluorescence microscopy as they tend to have short Stokes shifts, restricting the number of fluorophores that can be detected in a single sample to four to five. Herein, we synthesized a library of 95 novel boron-dipyrromethene (BODIPY)-based fluorophores and screened their photophys., optical and spectral properties for their utility in multicolor microscopy. A subset of our BODIPY-based fluorophores yielded varied length Stokes shifts probes, which were used to create a five-color image using a single excitation with confocal laser scanning microscopy for the first time. Combining these novel fluorophores with conventional fluorophores could facilitate imaging in up to nine to ten colors using linear unmixing based microscopy approaches.

Scientific Reports published new progress about Biological imaging. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, SDS of cas: 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Desai, Ranjit C. published the artcile5-Aryl thiazolidine-2,4-diones: discovery of PPAR dual α/γ agonists as antidiabetic agents, Category: chlorides-buliding-blocks, the main research area is thiazolidinedione derivative preparation structure activity peroxisome proliferator receptor antidiabetic.

A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARα/γ agonists was identified. A number of highly potent and orally bioavailable analogs were synthesized. Efficacy study results of some of these analogs in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics