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Synthesis of 3,4,5-trisubstituted isoxazoles in water via a [3 + 2]-cycloaddition of nitrile oxides and 1,3-diketones, β-ketoesters, or β-ketoamides [PDF]

open access: yesBeilstein Journal of Organic Chemistry, 2022
Herein we report a method for the synthesis of 3,4,5-trisubstituted isoxazoles in water under mild basic conditions at room temperature via a [3 + 2]-cycloaddition of nitrile oxides and 1,3-diketones, β-ketoesters, or β-ketoamides.
Md Imran Hossain   +3 more
doaj   +3 more sources

Trifluoromethylated Flavonoid-Based Isoxazoles as Antidiabetic and Anti-Obesity Agents: Synthesis, In Vitro α-Amylase Inhibitory Activity, Molecular Docking and Structure–Activity Relationship Analysis

open access: yesMolecules, 2021
Diabetes mellitus is a major health problem globally. The management of carbohydrate digestion provides an alternative treatment. Flavonoids constitute the largest group of polyphenolic compounds, produced by plants widely consumed as food and/or used ...
Faisal K. Algethami   +6 more
doaj   +2 more sources

Gold-Catalyzed Cyclization of Yndiamides with Isoxazoles via α-Imino Gold Fischer Carbenes. [PDF]

open access: yesChemistry, 2023
Gold catalysis is an important method for alkyne functionalization. Here we report the gold-catalyzed formal [3+2] aminative cyclization of yndiamides and isoxazoles in a direct synthesis of polysubstituted diaminopyrroles, which are important motifs in ...
Tong Z   +4 more
europepmc   +3 more sources

Ring-Opening Fluorination of Isoxazoles

open access: yesOrganic Letters, 2022
A ring-opening fluorination of isoxazoles has been developed. By treating isoxazoles with an electrophilic fluorinating agent (Selectfluor®), fluorination followed by deprotonation leads to tertiary fluorinated carbonyl compounds. The present method features mild reaction conditions, good functional group tolerance, and simple experimental procedure ...
Masaaki Komatsuda   +4 more
openaire   +3 more sources

Acridine–Isoxazole and Acridine–Azirine Hybrids: Synthesis, Photochemical Transformations in the UV/Visible Radiation Boundary Region, and Anticancer Activity [PDF]

open access: yesMolecules
Easy-to-handle N-hydroxyacridinecarbimidoyl chloride hydrochlorides were synthesized as convenient nitrile oxide precursors in the preparation of 3-(acridin-9/2-yl)isoxazole derivatives via 1,3-dipolar cycloaddition with terminal alkynes, 1,1 ...
Ekaterina E. Galenko   +3 more
doaj   +2 more sources

Synthesis of 2H-azirine-2,2-dicarboxylic acids and their derivatives [PDF]

open access: yesBeilstein Journal of Organic Chemistry
Methods for the preparation of 3-aryl-2H-azirine-2,2-dicarboxylic acids and their amides, esters, and azides by FeCl2-catalyzed isomerization of 3-aryl-5-chloroisoxazole-4-carbonyl chlorides into 3-aryl-2H-azirine-2,2-dicarbonyl dichlorides followed by ...
Anastasiya V. Agafonova   +2 more
doaj   +2 more sources

ISOXAZOLE–A POTENT PHARMACOPHORE [PDF]

open access: yesInternational Journal of Pharmacy and Pharmaceutical Sciences, 2017
Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib.
Chikkula, Krishna Veni, S., Raja
core   +5 more sources

Isoxazole Derivatives as Regulators of Immune Functions [PDF]

open access: yesMolecules, 2018
In this review, we present reports on the immunoregulatory properties of isoxazole derivatives classified into several categories, such as immunosuppressive, anti-inflammatory, immunoregulatory, and immunostimulatory compounds.
Michał Zimecki   +2 more
doaj   +3 more sources

Effects of Isoxazolyl Steroids on Key Genes of Sonic Hedgehog Cascade Expression in Tumor Cells [PDF]

open access: yesMolecules
Activation of the Hedgehog (Hh) signaling pathway is often associated with the progression of various types of cancer. The purpose of study was to search for inhibitors of the Hh signaling pathway among eight compounds belonging to the group of ...
Anna Aleksandrova   +10 more
doaj   +2 more sources

Isoxazole/Isoxazoline Skeleton in the Structural Modification of Natural Products: A Review

open access: yesPharmaceuticals, 2023
Isoxazoles and isoxazolines are five-membered heterocyclic molecules containing nitrogen and oxygen. Isoxazole and isoxazoline are the most popular heterocyclic compounds for developing novel drug candidates.
Xiyue Wang   +3 more
doaj   +1 more source

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