Awesome and Easy Science Experiments about 2682-49-7

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Docking assisted design of novel 4-adamantanyl-2-thiazolylimino-5-arylidene-4-thiazolidinones as potent NSAIDs$

Docking analysis was used to predict the effectiveness of adamantanyl insertion in improving cycloxygenase/lipoxygenase (COX/LOX) inhibitory action of previously tested 2-thiazolylimino-5-arylidene-4-thiazolidinones. The crystal structure data of human 5-LOX (3O8Y), ovine COX-1 (1EQH) and mouse COX-2 (3ln1) were used for docking analysis. All docking calculations were carried out using AutoDock 4.2 software. Following prediction results, 11 adamantanyl derivatives were synthesized and evaluated for biological action. Prediction evaluations correlated well with experimental biological results. Comparison of the novel adamantanyl derivatives with the 2-thiazolylimino-5-arylidene-4-thiazolidinones previously tested showed that insertion of the adamantanyl group led to the production of more potent COX-1 inhibitors, as well as LOX inhibitors (increased activity from 200% to 560%). Five compounds out of the 11 exhibited better activity than naproxen; while nine out of 11 showed better activity than NDGA and seven compounds possessed better anti-inflammatory activity than indomethacin.

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Awesome and Easy Science Experiments about 2682-49-7

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Synthesis, characterization and acute anti-inflammatory evaluation of new mefenamic acid derivatives having 4-thiazolidinone nucleus

Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug’s potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: Acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect. If you are interested in 2682-49-7, you can contact me at any time and look forward to more communication. COA of Formula: C3H5NOS

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Discovery of 2-Cyanoimino-1,3-thiazolidine

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3 – (2, 6 – Difluorophenyl) – 1, 2, 4 – oxdiazole compound and use thereof (by machine translation)

The present invention provides a 3 – (2, 6 – difluorophenyl) – 1, 2, 4 – oxdiazole compound miticides, the structure as shown in formula I: In the formula R is selected from: The formula I compound has excellent insecticidal or acaricidal activity, can be used for agriculture or forestry common pest control of mites. (by machine translation)

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Archives for Chemistry Experiments of Thiazolidin-2-one

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Acid-Catalyzed Synthesis of Thiazolidin-4-ones

A two-steps synthesis of thiazolidin-4-ones, from alpha-tetralone 6 or thiochroman-4-one 7, catalyzed by acids is described. The reactions of alpha-tetralone 6 or thiochroman-4-one 7, with substituted thiosemicarbazides, under AcOH or heteropolyacid (HPAs) catalysis afford thiosemicarbazones 8 and 9 in excellent yields. Condensations of the previous compounds 8 and 9 with alpha-bromoester, under sulfuric acid or heteropolyacid catalysis, yield the corresponding thiazolidin-4-ones 10 and 11.

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The important role of 2-Cyanoimino-1,3-thiazolidine

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 26364-65-8, name is 2-Cyanoimino-1,3-thiazolidine, introducing its new discovery. COA of Formula: C4H5N3S

2,2-Dialkylnaphthalen-1-ones as new potassium channel activators

A new series of 2,2-dialkylnaphthalen-1-one potassium channel activators has been prepared, and their in vitro relaxant activities in isolated rat portal vein and guinea pig tracheal spirals as well as their oral antihypertensive effect in spontaneously hypertensive rats have been evaluated. The group of 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2- dimethylnaphthalen-1-ones with an electron-withdrawing substituent at the 6- position contain the most active compounds and 1,2-dihydro-4-(1,2-dihydro-2- oxo-1-pyridyl)-2,2-dimethyl-1-oxonaphthalene-6-carbonitrile, 17f (UR-8225), has been selected for further pharmacological development.

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Discovery of 1,1-Dioxo-isothiazolidine

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BENZAZEPINE DERIVATIVES AS HISTAMINE H3 ANTAGONISTS

The present invention relates to novel benzazepine derivatives of structure (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. These compounds act as histamine H3 antagonists.

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Awesome Chemistry Experiments For Thiazolidin-2-one

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Crystal structure of methyl (Z)-2-[(Z)-3-methyl-2-({(E)-1-[(R ?)-4-methylcyclohex-3-en-1-yl]ethylidene}hydrazinylidene)-4-oxothiazolidin-5-ylidene]acetate

The new title 4-thiazolidinone derivative, C 16 H 21 N 3 O 3 S, was obtained from the cyclization reaction of 4-methyl-3-thiosemicarbazone and dimethyl acetylenedicarboxylate (DMAD). The cyclohexylidene ring has an envelope conformation with the stereogenic centre C atom as the flap. Its mean plane makes a dihedral angle of 56.23(9) with the thiazolidine ring mean plane. In the crystal, molecules are linked by C – H?O hydrogen bonds forming chains propagating in the [001] direction. Within the chains there are offset pi-pi interactions between the thiazolidine rings of inversion-related molecules [centroid-centroid distance = 3.703(1)A]. The chains are linked by further C – H?O hydrogen bonds, forming slabs parallel to the ac plane.

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New explortion of 2-Cyanoimino-1,3-thiazolidine

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Related Products of 26364-65-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.26364-65-8, Name is 2-Cyanoimino-1,3-thiazolidine, molecular formula is C4H5N3S. In a article£¬once mentioned of 26364-65-8

A including fluorine cyanogen imine thiazolidine substituted wicked two zuozuo kinds insecticide (by machine translation)

The present invention provides a including fluorine cyanogen imine thiazolidine substituted wicked two zuozuo kinds insecticide, the structure shown in formula I: The formula I compound Diamondback moth, Spodoptera exigua insecticidal, rice and the galenical, hot pepper anthrax bacteria, rice sheath blight fungus, Chinese rose inhibition of downy mildew and the like, can be used as agricultural or forestry plant pest control of the saw. (by machine translation)

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Brief introduction of Thiazolidin-2-one

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A NEW SYNTHESIS OF HETEROCYCLES VIA CARBONILATION OF AMINES WITH CARBON MONOXIDE IN THE PRESENCE OF SELENIUM

Amines which contain a second functional group in the appropriate position react with carbon monoxide in the presence of selenium to form heterocyclic derivatives in which carbon monoxide is incorporated.For instance, diamines, aminoalcohols, and their related compounds undergo carbonylation to give cyclic ureas, urethanes and the corresponding carbonylated compounds.For diamines and amino alcohols with more than two carbon atoms between the functional groups, intermolecular carbonylative coupling takes place competing with the intramolecular reaction.High selectivity has been attained under specified reaction conditions.Anilines having cyano or acetyl groups on the ortho position afford new classes of selenium-containing heterocycles.In these reactions, carbamoselenoate has been suggested as the common key intermediate.

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Properties and Exciting Facts About Thiazolidin-2-one

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Concise and Additive-Free Click Reactions between Amines and CF3SO3CF3

Trifluoromethyl trifluoromethanesulfonate has proved to be an excellent reservoir of difluorophosgene and a promising click ligation for amines in the preparation of urea derivatives, heterocycles, and carbamoyl fluorides under metal- and additive-free conditions. The reactions are rapid, efficient, selective, and versatile, and can be performed in benign solvents, giving products in excellent yields with minimal efforts for purification. The characteristics of the reactions meet the requirements of a click reaction. The use of trifluoromethyl trifluoromethanesulfonate as a click reagent is advantageous over other ?CO? sources (e.g., TsOCF3, PhCO2CF3, CsOCF3, AgOCF3, and triphosgene) because this reagent is readily accessible; easy to scale up; and highly reactive, even under metal- and additive-free conditions. It is anticipated that CF3SO3CF3 will be increasingly as important as SO2F2 as a click agent in future drug design and development.

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