Tag: M.W:100-200

Electric Literature of 90-64-2, 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. 90-64-2, Name is 2-Hydroxy-2-phenylacetic acid, SMILES is C1=CC=CC=C1C(C(O)=O)O, belongs to phthalazines compound. In a article, author is Abbasi, Marzieh, introduce new discover of the category.

Synthesis, characterization and in vitro antibacterial activity of novel phthalazine sulfonamide derivatives

Several phthalazine derivatives were synthesized by the one-pot three-component condensation in good to high yields in the presence of diatomite-SO3H as a solid acid catalyst. Then, a series (n= 14) of phthalazine sulfonamides were synthesized by the reaction phthalazine sulfonyl chloride and various amines under solvent-free conditions. The prepared compounds were screened for antibacterial activity against Escherichia coli (E. coli ATCC 25922) and Staphylococcus aureus (S. aureus ATCC 5213) as gram negative and positive respectively. Also, in silico physicochemical parameters of synthesized compounds were studied to predict absorption and permeability using Molinspiration online property calculation server.

Electric Literature of 90-64-2, 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 90-64-2 is helpful to your research.

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. 611-73-4, Name is 2-Oxo-2-phenylacetic acid, molecular formula is , belongs to phthalazines compound. In a document, author is Reilly, Sean W., Name: 2-Oxo-2-phenylacetic acid.

Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity

Development of poly(ADP-ribose) polymerase inhibitors (PARPi’s) continues to be an attractive area of research due to synthetic lethality in DNA repair deficient cancers; however, PARPi’s also have potential as therapeutics to prevent harmful inflammation. We investigated the pharmacological impact of incorporating spirodiamine motifs into the phthalazine architecture of FDA approved PARPi olaparib. Synthesized analogues were screened for PARP-1 affinity, enzyme specificity, catalytic inhibition, DNA damage, and cytotoxicity. This work led to the identification of 10e (12.6 +/- 1.1 nM), which did not induce DNA damage at similar drug concentrations as olaparib. Interestingly, several worst in class compounds with low PARP-1 affinity, including 15b (4397 +/- 1.1 nM), induced DNA damage at micromolar concentrations, which can explain the cytotoxicity observed in vitro. This work provides further evidence that high affinity PARPi’s can be developed without DNA damaging properties offering potential new drugs for treating inflammatory related diseases.

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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 623-25-6, Name is ¦Á,¦Á’-Dichloro-p-xylene, molecular formula is C8H8Cl2. In an article, author is Liu, Da-Chuan,once mentioned of 623-25-6, Product Details of 623-25-6.

Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives

The transcription factor nuclear factor-kappa B (NF-kappa B) controls many physiological processes including inflammation, immunity, and apoptosis. In this study, a novel series of 6-phenoxy-[1,2,4] triazolo[3,4-a] phthalazine-3-carboxamide derivatives were synthesized as potent anti-inflammatory agents, which acted on tumor necrosis factor (TNF-alpha) as inhibitors of NF-kappa B activation. We showed that compounds 6h (6-(2,4-dichlorophenoxy)-[1,2,4] triazolo[3,4-a] phthalazine-3-carboxamide) and 6i (6-(3-tolyloxy)[1,2,4] triazolo[3,4-a]phthalazine-3-carboxamide) showed more prominent anti-inflammatory activity than other compounds, with similar activities as the reference drug dihydrotanshinone; compound 6i showed the lowest cellular toxicity among the tested compounds. In vivo evaluation of the anti-inflammatory activity showed that compound 6i exhibited excellent anti-inflammatory activity with 58.19% inhibition at 50 mg/kg intraperitoneal (i.p.), with equal efficacy as the positive control indomethacin (100 mg/kg i.p.; 59.21% inhibition). (C) 2016 Elsevier Ltd. All rights reserved.

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

Electric Literature of 83-38-5, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 83-38-5, Name is 2,6-Dichlorobenzaldehyde, SMILES is C1=CC=C(C(=C1Cl)C=O)Cl, belongs to phthalazines compound. In a article, author is Taslimi, Parham, introduce new discover of the category.

2H-Indazolo[2,1-b]phthalazine-trione derivatives: Inhibition on some metabolic enzymes and molecular docking studies

In this study, substituted 2H-indazolo[2,1-b]phthalazine-1,6,11-trione compounds (4a-d) obtained via one-pot three-component condensation reaction of aromatic aldehydes, cyclic 1,3-dione, and phthalhydrazide in ethanol catalyzed by Y(OTf)(3) showed satisfactory inhibitory effects against some important enzymes. Also, these molecules had K-i values in the row of 185.92 +/- 36.03-294.82 +/- 50.76 nM vs carbonic anhydrase I (CA I), 204.93 +/- 46.90-374.10 +/- 83.63 nM against human CA II, 937.16 +/- 205.82-1021.83 +/- 193.66 nM against alpha-glycosidase (alpha-Gly), respectively. For cholinesterase enzymes, the K-i values were found in the range of 47.26 +/- 9.62-72.05 +/- 19.47 nM against acetylcholinesterase (AChE) and 65.03 +/- 9.88-102.83 +/- 25.04 nM against butyrylcholinesterase (BChE), respectively. The inhibition effects of these compounds against enzymes whose name are AChE, BChE, alpha-Gly, hCA I, and hCA II, were compared with control molecules like tacrine, acarbose, and acetazolamide.

Electric Literature of 83-38-5, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 83-38-5.

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. Name: Diphenylsilane, 775-12-2, Name is Diphenylsilane, SMILES is C1([SiH2]C2=CC=CC=C2)=CC=CC=C1, in an article , author is Zhang, Qiu-Rong, once mentioned of 775-12-2.

Synthesis and antimicrobial activities of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives

A series of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives were synthesized in five steps from a common precursor, phthalic anhydride. Most of synthesized phthalazine derivatives showed inhibitory activity against Staphylococcus aureus. One of phthalazine derivatives 5l showed inhibitory activity against all tested bacterial and fungal strains. (C) 2014 Published by Elsevier Ltd.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 775-12-2, you can contact me at any time and look forward to more communication. Name: Diphenylsilane.

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. 140-75-0, Name is (4-Fluorophenyl)methanamine, molecular formula is , belongs to phthalazines compound. In a document, author is Gao, Cheng-Zhi, Recommanded Product: 140-75-0.

Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors

A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 +/- 1.25 nM) and MDA-MB-436 cancer cell (11.62 +/- 2.15 mu M), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer’s disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 +/- 0.91 mu M) which was stronger than neostigmine (12.01 +/- 0.45 mu M) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer’s disease.

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 140-75-0, in my other articles. Recommanded Product: 140-75-0.

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

Reference of 1821-12-1, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 1821-12-1, Name is 4-Phenylbutanoic acid, SMILES is O=C(O)CCCC1=CC=CC=C1, belongs to phthalazines compound. In a article, author is Bolteau, Raphael, introduce new discover of the category.

Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine

For further development of successors of Agomelatine through modulation of its pharmacokinetic properties, we report herein the design, synthesis and pharmacological results of a new family of melatonin receptor ligands. Issued from the introduction of quinazoline and phthalazine scaffolds carrying an ethyl amide lateral chain and a methoxy group as bioisosteric ligands analogues of previously developed Agomelatine. The biological activity of the prepared analogues was compared with that of Agomelatine. Quinazoline and phthalazine rings proved to be a versatile scaffold for easy feasible MT1 and MT2 ligands. Potent agonists with sub-micromolar binding affinity were obtained. However, the presence of two nitrogen atoms resulted in compounds with lower affinity for both MT1 and MT2, in comparison with the parent compound, balanced by the exhibition of good pharmacokinetic properties. (C) 2020 Elsevier Masson SAS. All rights reserved.

Reference of 1821-12-1, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 1821-12-1 is helpful to your research.

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

Reference of 1571-08-0, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 1571-08-0, Name is Methyl 4-formylbenzoate, SMILES is C1=C(C(OC)=O)C=CC(=C1)C=O, belongs to phthalazines compound. In a article, author is Reddy, Mudumala Veeranarayana, introduce new discover of the category.

InCl3-catalyzed green synthesis of 1H-pyrazolo[1,2-b]phthalazine-5,10-diones under solvent-free conditions

A simple, efficient, and green practical approach to 1H-pyrazolo[1,2-b]phthalazine-5,10-diones from phthalhydrazide, aldehydes, and malononitrile/ethyl cyanoacetate has been developed that uses inexpensive and readily available InCl3 as a catalyst in solvent-free one-pot three-component cyclo condensation reaction. This method should provide high yields, shorter reaction time, easy work-up, purification of products by nonchromatographic method, and cleaner reaction. It is a new strategy for N-fused heterocycles synthesis, which haswider application in organic and medicinal chemistry. (c) 2013 Elsevier Ltd. All rights reserved.

Reference of 1571-08-0, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 1571-08-0.

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

Reference of 619-67-0, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 619-67-0, Name is 4-Hydrazinylbenzoic acid, SMILES is O=C(O)C1=CC=C(NN)C=C1, belongs to phthalazines compound. In a article, author is El-Shamy, Ibrahim E., introduce new discover of the category.

Synthesis of Some Biologically Active Pyrazolylphthalazine Derivatives and Acyclo-C-nucleosides of 6-(2,4,6-trimethylphenyl)-1,2,4-triazolo[3,4-a]phthalazine

1-Chloro-4-(2,4,6-trimethylphenyl) phthalazine (2) was used as a precursor for preparation of some novel pyrazolylphthalazine derivatives 6-13 and 15-19. Moreover, the acyclonucleosides 20-23 a-e were prepared by the reaction of hydrazinophthalazine derivative 3 with different aldoses. All new phthalazine derivatives were characterized using H-1 NMR, C-13 NMR, FTIR, mass spectrum and elemental analysis. The newly synthesized compounds showed highly activity against different species of bacteria and fungi, in addition to an excellent antiinflammatory property.

Reference of 619-67-0, 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 619-67-0 is helpful to your research.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 103-45-7, Name is Phenethyl acetate, formurla is C10H12O2. In a document, author is Patil, Smita, introducing its new discovery. Application In Synthesis of Phenethyl acetate.

A novel phthalazine based highly selective chromogenic and fluorogenic chemosensor for Co2+ in semi-aqueous medium: application in cancer cell imaging

A new phthalazine based chemosensor 3 was developed for the highly selective and sensitive detection of Co2+ in the mixed solvent system, CH3CN- H2O ( 1 : 1, v/ v). In the presence of Co2+, the colour of the solution 3 changed from yellow to green; the absorption maxima of 3 was red- shifted from 383 nm to 435 nm, and the fluorescence of 3 at 550 nm was significantly enhanced. The sensor 3 showed a detection limit down to 25 nM by forming a complex species with Co2+ in 1 : 1 stoichiometry. Furthermore, by means of confocal laser scanning microscopy experiments, it has demonstrated that it can be used as a fluorescent probe for monitoring Co2+ in living cells.

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