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1-(5-(R-Amino)-1,2,4-thiadiazol-3-yl)propan-2-ones: Convenient ketomethylenic reagents for the gewald and dimroth reactions

1-(5-(R-Amino)-1,2,4-thiadiazol-3-yl)propan-2-ones were used as activated ketomethylenic compounds for the Gewald and Dimroth reactions. It was found out that they exhibited high reactivity in such anion reactions for the construction of the 1,2,3-triazole and thiophene frameworks. The target 1,2,3-triazoles and thiophenes were obtained in high yields in minimum time.

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Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Sulfamethoxazole degradation by ultrasound/ozone oxidation process in water: Kinetics, mechanisms, and pathways

In this research, sulfamethoxazole (SMX) degradation was investigated using ultrasound (US), ozone (O3) and ultrasound/ozone oxidation process (UOOP). It was proved that ultrasound significantly enhanced SMX ozonation by assisting ozone in producing more hydroxyl radicals in UOOP. Ultrasound also made the rate constants improve by kinetics analysis. When ultrasound was added to the ozonation process, the reaction rate increased by 6-26% under different pH conditions. Moreover, main intermediates oxidized by US, O3 and UOOP system were identified. Although the main intermediates in ozonation and UOOP were similar, the introduction of ultrasound in UOOP had well improved the cleavage of S-N bond. In this condition SMX become much easier to be attacked, which led to enhanced SMX removal rate in UOOP compared to the other two examined processes. Finally, the SMX degradation pathways were proposed.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Antibacterial activity of sulfamethoxazole transformation products (TPs): General relevance for sulfonamide TPs modified at the para position

Sulfonamide antibiotics undergo transformation in the aquatic environment through biodegradation, photolysis, or hydrolysis. In this study, the residual antibacterial activity of 11 transformation products (TPs) of sulfamethoxazole (SMX) was investigated with regard to their in vitro growth and luminescence inhibition on Vibrio fischeri (30 min and 24 h exposure). Two transformation products, 4-hydroxy-SMX and N4-hydroxy-acetyl-SMX, were synthesized in-house and confirmed by nuclear magnetic resonance and high-resolution mass spectrometry. Results of individual compound experiments showed that TPs modified at the para amino group still exhibit clear antibacterial effects, whereas TPs resulting from breakdown of the SMX structure lost this mechanism of action. 4-NO2- and 4-OH-SMX were found to inhibit growth to a clearly greater extent than the parent compound, SMX. In contrast, the N4-acetyl- and N4-hydroxy-acetyl-derivatives retain less than 10 and 5% of the effect of SMX on growth and luminescence inhibition, respectively. The effect of a mixture of para-modified TPs was observed to be additive. Considering the homologous series of sulfa drugs widely prescribed and their common mechanism of action, the potential environmental impact must consider the total amount of sulfonamide antibiotics and their derivative TPs, which might end up in a water body. Extrapolating the results obtained here for the para TPs of SMX to other sulfa drugs and determining the persistence and occurrence of these compounds in the aquatic environment is required for improved risk assessment. (Chemical Equation Presented).

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Direct reductive aminations with catalytic molybdenum dioxide dichloride and phenylsilane

A powerful direct reductive amination (DRA) method is developed, using catalytic MoO2Cl2 and phenylsilane (PhSiH3) as the reducing agent. The alkylation of a range of amines (pKa 0-7.8) with both an electron-deficient and two electron-rich-aldehydes is achieved in good to excellent yields. The novel employment of this DRA in alcoholic solvents significantly improves the reaction scope and excellent functional group selectivity is exhibited.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Synthesis and in vitro study of novel isoxazolyl benzoimidazolyl benzamides, acrylamides and propionamides as antimicrobial agents

A series of novel 2/3 (1H-benzoimidazol-2-yl)-N-(5-methyl-3-isoxazolyl)- benzamides, acrylamides and propionamides have been synthesized and the antimicrobial activities are evaluated against two Gram-positive and two Gram-negative bacteria and two plant-pathogenic fungi. Some of the synthesized compounds have showed superior in vitro activities as compared to the standard drugs.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Microwave-induced acetoacetylation of isoxazolyl amines with beta-keto esters

The reaction of isoxazolyl amines with different beta-keto esters under microwave irradiation, without using any catalyst and/or solvent leads to the formation of isoxazolyl amide derivatives by acetoacetylation.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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A Convenient and Facile Hantzsch Synthesis of Aryl Imidazo[1,2-b]Isoxazolyl-N-aryl Thiazol Amines

The Hantzsch synthesis of novel aryl imidazo[1,2-b]isoxazolyl-N-aryl thiazol amines 5 analogues were described. Reaction of 3-aminoisoxazole 1 with substituted phenacyl bromides 2 in dry ethanol afforded the corresponding 6-methyl-3-arylimidazo[1,2-b]isoxazoles 3 in good yields. Compounds 3 on reaction with chloroacetyl chloride in 1,4-dioxane furnished the corresponding 2-chloro-1-(6-methyl-3-arylimidazo[1,2-b]isoxazol-2-yl)ethanones 4. Compounds 4 on heating with N-aryl thioureas in an oil bath underwent cyclization to afford the title compounds viz., imidazo[1,2-b]isoxazolyl-N-aryl thiazol amines 5 in moderate to good yields by Hantzsch synthesis.

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Isoxazole – Wikipedia,
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1-aryl-3-quinolinecarboxamide

Novel 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides, processes for the preparation thereof, and methods for treating pain and inflammation utilizing compounds and compositions thereof are disclosed.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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NOVEL DUAL ACTION RECEPTORS ANTAGONISTS (DARA) AT THE AT1 AND ETA RECEPTORS

The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2- thiophenecarboxamides as selective endothelin receptor-A antagonists

We report here that N2-aryl-3-(isoxazolylsulfamoyl)-2- thiophenecarboxamides are potent and selective small molecule ET(A) receptor antagonists. The aryl group was subjected to extensive structural modification. With monosubstitution, the para position was most useful in increasing potency, with methyl being preferred. With disubstitution, 2,4- disubstitution further enhanced activity with methyl or cyano groups being preferred at the 2-position. In this series, a benzo[d][1,3]dioxole group is equivalent to a 4-methyl group in in vitro activity and afforded the compounds with both in vivo activity and moderate half-lives.

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Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem