Category: 139-66-2

Synthetic Route of 139-66-2, Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 139-66-2, Name is Diphenylsulfane, SMILES is C1(SC2=CC=CC=C2)=CC=CC=C1, belongs to phthalazine compound. In a article, author is Takaoka, Naoki, introduce new discover of the category.

As aldehyde oxidase (AOX) plays an emerging role in drug metabolism, understanding its significance for drug-drug interactions (DDI) is important. Therefore, we tested 10 compounds for species-specific and substrate-dependent differences in the inhibitory effect of AOX activity using genetically engineered HEK293 cells over- expressing human AOX1, mouse AOX1 or mouse AOX3 The IC50 values of 10 potential inhibitors of the three AOX enzymes were determined using phthalazine and O-6-benzylguanine as substrates 17 beta-Estradiol, mena dione, norharmane and raloxifene exhibited marked differences in inhibitory effects between the human and mouse AOX isoforms when the phthalazine substrate was used. Some of the compounds tested exhibited substrate dependent differences m their inhibitory effects. Docking simulations with human AOX1 and mouse AOX3 were conducted for six representative inhibitors. The rank order of the minimum binding energy reflected the order of the corresponding IC50 values. We also evaluated the potential DDI between an AOX substrate (O-6-benzylguanine) and an inhibitor (hydralazine) using chimeric mice with humanized livers. Pretreatment of hydralazine increased the maximum plasma concentration (C-max) and the area under the plasma concentration- time curve (AUC(0-24)) of O-6-benzylguanine compared to single administration. Our in vitro data indicate species-specific and substrate-dependent differences in the inhibitory effects on AOX activity. Our in vivo data demon strate the existence of a DDI which may be of relevance in the clinical context.

Synthetic Route of 139-66-2, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 139-66-2.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

In an article, author is Chang, Sue-Ming, once mentioned the application of 139-66-2, Name is Diphenylsulfane, molecular formula is C12H10S, molecular weight is 186.2728, MDL number is MFCD00003064, category is phthalazine. Now introduce a scientific discovery about this category, COA of Formula: https://www.ambeed.com/products/139-66-2.html.

Hybrid molecules are composed of two pharmacophores with different biological activities. Here, we conjugated phthalazine moieties (antiangiogenetic pharmacophore) and bis(hydroxymethyl)pyrrole moieties (DNA cross-linking agent) to form a series of bis(hydroxymethyl)pyrrolo[2,1-a]phthalazine hybrids. These conjugates were cytotoxic to a variety of cancer cell lines by inducing DNA damage, arresting cell cycle progression at the G2/M phase, triggering apoptosis, and inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2) in endothelial cells. Among them, compound 29d encapsulated in a liposomal formulation (e.g., 29dL) significantly suppressed the growth of small-cell lung cancer cell (H526) xenografts in mice. Based on immunohistochemical staining, the tumor xenografts in mice treated with 29dL showed time-dependent decreases in the intensity of CD31, a marker of blood vessels, whereas the intensity of gamma-H2AX, a marker of DNA damage, increased. The present data revealed that the conjugation of antiangiogenic and DNA-damaging agents can generate potential hybrid agents for cancer treatment.

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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 139-66-2, Name is Diphenylsulfane, molecular formula is C12H10S. In an article, author is Kerru, Nagaraju,once mentioned of 139-66-2, SDS of cas: 139-66-2.

An eco-friendly and efficient green protocol is developed for the synthesis of sixteen pyrazolo-phthalazine derivatives (5a-p) by using inexpensive biodegradable eggshell powder (ESP) as a heterogeneous catalyst. The four-component one-pot condensation reaction proceeded through Knoevenagel-Michael reaction of different chosen active methylene compounds, phthalic anhydride, and hydrazine hydride with various substituted aromatic aldehydes in the water at 60 degrees C, and furnished the high yields of products (93-98%) in rapid reaction time of 28 to 45 min. The material was characterized by different analytical techniques (SEM, TEM, XRD, BET, and FT-IR), and was composed of the high percentage of calcium oxides and carbonates, and less percentage of Na and Mg elements (based on EDX analysis). The ESP material displayed recyclability (4 times) without any notable loss of catalytic efficacy. Besides, this procedure offers 98% of the atom economy and 100% of carbon efficiency together with significant fiscal and enviro-friendly benefits.

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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 139-66-2, Name is Diphenylsulfane, SMILES is C1(SC2=CC=CC=C2)=CC=CC=C1, in an article , author is Kumar, P. Sagar Vijay, once mentioned of 139-66-2, HPLC of Formula: https://www.ambeed.com/products/139-66-2.html.

A series of novel chromeno-pyrazolo[1,2-b] phthalazine-6,9,14(7H)-trione derivatives (4a-k) were designed and prepared using a reusable and efficient catalyst ionic liquid [Bmim] BF4 via one-pot multi-component reaction. Their bioactivity was evaluated against Aspergillus niger and Candida albicans in vitro. Compound 4f was found to be the most effective compared to all other synthesised compounds. To validate experimental biological data obtained, molecular docking study was carried out. It was observed that compound 4f showed stronger binding interactions with secreted aspartic proteinase (SAP) of C. albicans (1EAG). Further, primary optimisation of drug-like properties was studied through in silico predictions by using ADMET predictor FAF-drug2 and OSIRIS property explorer. (C) 2015 King Saud University. Production and hosting by Elsevier B.V.

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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Application of 139-66-2, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 139-66-2, Name is Diphenylsulfane, SMILES is C1(SC2=CC=CC=C2)=CC=CC=C1, belongs to phthalazine compound. In a article, author is Lu, Xiuhong, introduce new discover of the category.

We report herein the design and synthesis of a series of optimized phthalazine compounds as novel hedgehog signaling pathway inhibitors. The 4-methylamino-piperidine moiety of Taladegib was replaced by different four, five or six-membered azacycle or azaspirocycle building blocks. The in vitro Gliluciferase assay results demonstrate that the scaffold hopping in this region afforded significant influences on Hh pathway inhibition. Pyrrolidin-3-amine moiety was found to be the best linker between pharmacophores phthalazine and fluorine substituted benzoyl group. Meanwhile the optimization of 1-methyl-1H-pyrazol by different aromatic rings was also investigated and the SAR was described. Many new derivatives were found to show potent Hh signaling inhibitory activity with nanomolar IC50 values. Among these compounds, compound 23b showed the highest inhibitory potency with an IC50 value of 0.17 nM, which was 35-fold more potent than the lead compound Taladegib and 23-fold more potent than the marketed drug Vismodegib. The selected compounds 23a and 23b also possess potent antitumor activities against medulloblastoma cells proliferation in vitro. In vivo efficacy of 23b in a ptch(+/-)p53(-/-) mouse medulloblastoma allograft model also indicated encouraging results. (C) 2017 Elsevier Masson SAS. All rights reserved.

Application of 139-66-2, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 139-66-2 is helpful to your research.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, SDS of cas: 139-66-2139-66-2, Name is Diphenylsulfane, SMILES is C1(SC2=CC=CC=C2)=CC=CC=C1, belongs to phthalazine compound. In a article, author is Tuerkmen, Yunus E., introduce new discover of the category.

The first syntheses and structural elucidation of Ag(I) ternary complexes with 1,2-diazines and chelating heteroarenes have been described. Conserved modes of inter-cation Ag+…pi and pi…pi stacking interactions result in near identical patterns of cation self-assembly in these ternary complexes.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 139-66-2. SDS of cas: 139-66-2.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Chemistry can be defined as the study of matter and the changes it undergoes. You’ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 139-66-2, Name is Diphenylsulfane, molecular formula is , belongs to phthalazine compound. In a document, author is Liu, Honglei, SDS of cas: 139-66-2.

Sc(OTf)(3)-Catalyzed [3+3] Cycloaddition of Cyclopropane 1,1-Diesters with Phthalazinium Dicyanomethanides

The Sc(OTf)(3)-catalyzed diastereoselective [3 + 3] cycloaddition of phthalazinium dicyanomethanides with cyclopropane 1,1-diesters proceeded smoothly under mild reaction conditions, affording a variety of 3,4-dihydro-1H-pyrido[2,1-a]phthalazine derivatives in up to 99% yields with excellent diastereoselectivities.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 139-66-2, in my other articles. SDS of cas: 139-66-2.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 139-66-2, Name is Diphenylsulfane, molecular formula is C12H10S, belongs to phthalazine compound, is a common compound. In a patnet, author is Muddala, N. Prasad, once mentioned the new application about 139-66-2, Category: phthalazines.

Inhibitor design to target a unique feature in the folate pocket of Staphylococcus aureus dihydrofolate reductase

Staphylococcus aureus (Sa) is a serious concern due to increasing resistance to antibiotics. The bacterial dihydrofolate reductase enzyme is effectively inhibited by trimethoprim, a compound with antibacterial activity. Previously, we reported a trimethoprim derivative containing an acryloyl linker and a dihydophthalazine moiety demonstrating increased potency against S. aureus. We have expanded this series and assessed in vitro enzyme inhibition (K-i) and whole cell growth inhibition properties (MIC). Modifications were focused at a chiral carbon within the phthalazine heterocycle, as well as simultaneous modification at positions on the dihydrophthalazine. MIC values increased from 0.0626-0.5 mu g/mL into the 0.5-1 mu g/mL range when the edge positions were modified with either methyl or methoxy groups. Changes at the chiral carbon affected K-i measurements but with little impact on MIC values. Our structural data revealed accommodation of predominantly the S-enantiomer of the inhibitors within the folate-binding pocket. Longer modifications at the chiral carbon, such as p-methylbenzyl, protrude from the pocket into solvent and result in poorer K-i values, as do modifications with greater torsional freedom, such as 1-ethylpropyl. The most efficacious K-i was 0.7 +/- 0.3 nM, obtained with a cyclopropyl derivative containing dimethoxy modifications at the dihydrophthalazine edge. The co-crystal structure revealed an alternative placement of the phthalazine moiety into a shallow surface at the edge of the site that can accommodate either enantiomer of the inhibitor. The current design, therefore, highlights how to engineer specific placement of the inhibitor within this alternative pocket, which in turn maximizes the enzyme inhibitory properties of racemic mixtures. (C) 2020 Elsevier Masson SAS. All rights reserved.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 139-66-2. The above is the message from the blog manager. Category: phthalazines.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Related Products of 139-66-2, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 139-66-2, Name is Diphenylsulfane, SMILES is C1(SC2=CC=CC=C2)=CC=CC=C1, belongs to phthalazine compound. In a article, author is Kefayati, Hassan, introduce new discover of the category.

Electrocatalytic multicomponent assembling of phthalhydrazide, aldehydes and malononitrile: An efficient approach to 1H-pyrazolo[1,2-b]phthalazine-5,10-diones

Electrocatalytic multicomponent transformation of phthalhydrazide, aromatic aldehydes and malononitrile in n-propanol in an undivided cell in the presence of sodium bromide as an electrolyte leads to 1H-pyrazolo[1,2-b]phthalazine-5,10-diones in short reaction times (4-8 min) and high yields (85-98%) at room temperature. The developed efficient electrocatalytic approach to the corresponding 1H-pyrazolo[1,2-b]phthalazine-5,10-diones is beneficial from the viewpoint of diversity-oriented large-scale processes and represents a new example of the ecologically pure synthetic concept for electrocatalytic multicomponent reactions strategy. (C) 2013 Academie des sciences. Published by Elsevier Masson SAS. All rights reserved.

Related Products of 139-66-2, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 139-66-2 is helpful to your research.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem