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Novel 3,3a,4,5,6,7-Hexahydroindazole and Arylthiazolylpyrazoline derivatives as Anti-inflammatory Agents

A novel series of 7-benzylidene-3,3a,4,5,6, 7-hexahydro-3-phenyl-2H-indazole substituted at the 2-position were synthesized. The reaction of 2,6-bis-benzylidenecyclohexanone (1) with thiosemicarbazide in the presence of NaOH afforded a mixture of the 3-H, 3a-H trans 2 and cis 2a diastereoisomers which have been separated by fractional recrystallization. Interaction of the first intermediate 2 with substituted phenacyl bromides, aromatic aldehydes and chloroacetic acid in presence of a mixture of acetic acid and acetic anhydride, and 2,3-dichloroquinoxaline yielded the corresponding 7-benzylidene-3,3a,4,5,6,7-hexahydro-3-phenyl-2H-indazole derivatives substituted at the 2-position with 4-aryl-2-thiazolyl 3 a, b, 5-arylidene-4,5-dihydro-4-oxo-2-thiazolyl 4a, b and thiazolo[4,5-b]quinoxalin-2-yl 5, respectively. Moreover, the other intermediates 3,5-diaryl-1-thiocarbamoyl-2-pyrazolines 7 a-d were reacted with the previously-mentioned reagents and gave the corresponding 3,5-diaryl-1-(4-aryl-2-thiazolyl)-2-pyrazolines 8 a-h, 3,5-diaryl-1-(5-arylidene-4,5-dihydro-4-oxo-2-thiazolyl)-2-pyrazolines 9 a-d and 3,5-diaryl-1-(thiazolo[4,5-b]quinoxalin-2-yl)-2-pyrazoline derivatives 10 a, b, respectively. Some of the newly prepared compounds were subjected to evaluation for their anti-inflammatory activity. The structures of the new compounds were confirmed by elemental analyses as well as 1H-NMR, IR, and MS data.

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Awesome Chemistry Experiments For 3,4-Dihydroquinoxalin-2(1H)-one

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Synthesis and characterization of orally active nonpeptide vasopressin V2 receptor antagonists

The present study was undertaken to evaluate whether a novel series of 2,6-diaza-5-oxobicyclo[5.4.0]undeca-1(7),8,10-triene derivatives exhibited antagonistic activity for vasopressin V1 and V2 receptors. Most of these compounds were synthesized and showed a high affinity potential for V2 receptor and low to moderate affinity potential for V1 receptor. The most potent and V2-selective compound, N-[4-[2,6-diaza-6-[2-(4- methylpiperazinyl)-2-oxoethyl]-5-oxobicyclo [5.4.0] undeca-1 (7),8,10-trien- 2-yl]-carbonyl]phenyl] [2-(4-methylphenyl)phenyl]formamide (11b), exhibited IC50’s of 2.9 nM for the V2 receptor and 200 nM for the V1 receptor, respectively. When administered orally to rat, 11b showed an approximately 18-fold increased urine volume in comparison with control rat.

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Awesome and Easy Science Experiments about 5-Nitroquinoxaline

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Anticonvulsant evaluation of clubbed indole-1,2,4-triazine derivatives: A synthetic approach

A series of thirty indole C-3 substituted 5-amino-6-(5-substituted-2- phenyl-1H-indol-1-yl)-4,5-dihydro-1,2,4-triazine-3(2H)-thione 5a-f, 6a-f, 7a-f, 8a-f and 9a-f were synthesized to explore prospective anticonvulsant agents. The derivative 1-(1-(5-amino-3-thioxo-2,3,4,5-tetrahydro-1,2,4-triazin-6-yl)-5- fluoro-2-phenyl-1H-indol-3-yl)ethanone (6b) had significant activity in maximal electroshock test with minimal duration of limb extension (5.40 ¡À 0.61 s) and quantitative median dose of 7 mg/kg. In subcutaneous pentylenetetrazole screen 1-(5-amino-3-thioxo-2,3,4,5-tetrahydro-1,2,4-triazin-6-yl)-5-fluoro-2- phenyl-1H-indole-3-sulfonamide (7b) increased the seizure latency to onset of clonus and was effective at a median dose of 35 mg/kg. An in vitro radioligand binding assay on sodium channel and gamma-amino butyric acid estimation was also performed on active compounds to perceive the mechanistic procedure responsible for it action.

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Awesome and Easy Science Experiments about 7712-28-9

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Synthesis of hydrazones derivatives of quinoxalinone- prospective antimicrobial and antiinflammatory agents

A series of quinoxalinone derivatives was synthesized by the condensation of 1,2-diaminobenzene with alpha-ketoglutaric acid to yield 3-(3-oxo-3,4-dihydroquinoxalin-2-yl) propionic acid (2) and then treated with hydrazine hydrate to yield its hydrazones (3). This was further reacted with substituted aromatic aldehydes to produce final compounds (4a-r). These hydrazones derivatives were characterized by FT-IR and 1H-NMR data. All the synthesized compounds were evaluated for their antimicrobial and antiinflammatory activity.

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Archives for Chemistry Experiments of 2-Chloroquinoxaline

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Reference of 1448-87-9, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 1448-87-9, molcular formula is C8H5ClN2, introducing its new discovery.

Reactions of Organic Anions, 177. Vicarious Nucleophilic Substitution of Hydrogen, Bisannulation and Competitive Reactions of alpha-Haloalkyl Carbanions with Bicyclic Azaaromatic Compounds

Carbanions of alpha-haloalkyl aryl sulfones, sulfonates, and sulfonamides react with bicyclic heteroaromatic compounds (quinoxalines, naphthyridines, and 5-azaquinoxalines) according to two general pathways: vicarious nucleophilic substitution of hydrogen and/or bisannulation.In some cases other competitive reactions such as SNAr are observed.Factors governing the direction of these reactions are discussed in terms of the charge distribution in the anionic ? adducts and the reaction conditions.

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Archives for Chemistry Experiments of 2-Chloro-6-fluoroquinoxaline

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FIVE MEMBERED-AMINOHETEROCYCLIC AND 5,6-OR 6,6-MEMBERED BICYCLIC AMINOHETEROCYCLIC INHIBITORS OF ROCK FOR THE TREATMENT OF HEART FAILURE

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

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The Absolute Best Science Experiment for 15804-19-0

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Synthesis, Characterization and Antimicrobial Activity of 1,2-dihydroquinoxaline-3-yl-3-Substitutedphenyl-1H-pyrazole-4-Carbaldehyde

A series of 1,2-dihydroquinoxaline-3-yl-3-substitutedphenyl-1H-pyrazole-4-carbaldehyde were synthesized and evaluated for their antimicrobial activity against two Gram-positive and two Gram-negative organisms and two fungal organisms. The study has shown that pyrazole-4-carbaldehyde-incorporated quinoxaline was essential for activity. Among the compounds, 5a, 5c, 5d had shown significant activity against all selected strains when compared with control. These compounds may prove useful as antimicrobial agents.

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Discovery of Quinoxaline-2,3(1H,4H)-dione

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Mannich bases in medicinal chemistry and drug design

The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

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Final Thoughts on Chemistry for 2-Chloroquinoxaline

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Synthesis of (eta 5-cyclopentadienyl)-1-(4-benzyloxycarbonyl-3,4-dihydroquinoxalin-2- yl)ethene-1,2-dithiolatocobalt(III) and (eta 5-cyclopentadienyl)-1-[2-(N,N-dimethylaminomethyleneamino)-3-methyl- 4-oxopteridin-6-yl]ethene-1,2-dithiolatocobalt(III)

Cobalt(III) complexes are reported in which (a) a dihydroquinoxalinylethenedithiolate ligand models the pyrazine ring oxidation level in Moco, and (b) a pteridinylethenedithiolate models the pteridine ligand in Moco.

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A new application about 6-Nitroquinoxaline

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Hair dye compositions and certain 1,2,3,4-tetrahydronitroquinoxalines useful therein

The invention relates to the use of compounds corresponding to formula (I) STR1 in which one of the substituents R1 or R2 is a nitro group while the other is hydrogen, halogen, an amino group, a mono- or dialkylamino group containing C1-4 alkyl groups, a C1-4 alkyl or alkoxy group, R3 and R4 independently of one another represent hydrogen or a C1-4 alkyl group, A is a >CHR6 – or a >C=O- group, where R6 is hydrogen or a C1-4 alkyl group, and R5 is hydrogen or a C1-4 alkyl group, or salts thereof as substantive dyes in hair-dyeing compositions. When the substituent groups in formula I represent one of the combinations I-IV shown in the table below, the compounds are novel and are useful in hair-dyeing compositions. ______________________________________R1 R2 R3 R4 R5 A______________________________________I: H NO2 H CH3 H CH2II: H NO2 CH3 CH3 H CH2III: NH2 NO2 H H H CH2IV: H NO2 H H CH3 CH2.______________________________________

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