Kinetic Study on the Base-Catalyzed Imine-Enamine Tautomerism of a Chiral Biologically Active Isoxazoline Derivative by HPLC on Amylose Tris(3,5-dimethylphenylcarbamate) Chiral Stationary Phase [PDF]
Isoxazoline is a nitrogen- and oxygen-containing five-membered heterocyclic scaffold with diverse biological profiles such as antimicrobial, fungicidal, anticancer, antiviral, analgesic and anti-inflammatory activity.
Daniele Sadutto+4 more
doaj +2 more sources
New isoxazolidinyl-based N-alkylethanolamines as new activators of human brain carbonic anhydrases [PDF]
Carbonic anhydrases (CAs) are widespread metalloenzymes which catalyse the reversible hydration of carbon dioxide (CO2) to bicarbonate (HCO3−) and a proton, relevant in many physiological processes. In the last few years, the involvement of CA activation
Doretta Cuffaro+6 more
doaj +2 more sources
Synthesis and In Silico Analysis of New Polyheterocyclic Molecules Derived from [1,4]-Benzoxazin-3-one and Their Inhibitory Effect against Pancreatic α-Amylase and Intestinal α-Glucosidase [PDF]
This study focuses on synthesizing a new series of isoxazolinyl-1,2,3-triazolyl-[1,4]-benzoxazin-3-one derivatives 5a–5o. The synthesis method involves a double 1,3-dipolar cycloaddition reaction following a “click chemistry” approach, starting from the ...
Mohamed Ellouz+12 more
doaj +2 more sources
The use of isoxazoline and isoxazole scaffolding in the design of novel thiourea and amide liquid-crystalline compounds [PDF]
A series of novel thiourea and amide liquid crystals containing 5-membered isoxazoline and isoxazole rings were synthetized and the liquid crystal properties studied.
Itamar L. Gonçalves+3 more
doaj +2 more sources
The mosquitocidal activity of isoxazoline derivatives afoxolaner, lotilaner, and fluralaner are not affected by mosquito sugar or antibiotic treatment [PDF]
Long-lasting insecticidal nets and indoor residual sprays have played a major role in significantly reducing the burden of malaria. However, the management of mosquitoes resistant to current insecticides continues to be challenging.
Harouna Soré+8 more
doaj +3 more sources
Fecal elimination of fluralaner in different carnivore species after oral administration [PDF]
Fluralaner is a recent external parasiticide, first of a new class of drugs (isoxazoline parasiticides). It is widely used in companion animals both for its wide spectrum (fleas, ticks and other mites) but also for its ease of use (oral tablets given ...
Philippe Jacques Berny+3 more
doaj +2 more sources
Discovery of a Novel Class of Acylthiourea-Containing Isoxazoline Insecticides against Plutella xylostella [PDF]
Isoxazoline structures are widely found in natural products and are rich in biological activities. This study discloses the development of a series of novel isoxazoline derivatives by introducing acylthiourea fragments to access insecticidal activity ...
Fangyi Li+6 more
doaj +2 more sources
An Unexpected Formation of Spiro Isoxazoline-Dihydrofurane Compounds from Substituted Ketofurfuryl Alcohols [PDF]
Oximation of substituted ketofurfuryl alcohols in the presence of hydroxylamine hydrochloride and pyridine in ethanol as solvent led to a new class of spiro derivatives presenting a 7-methylene-1,6-dioxa-2-azaspiro [4.4] nona-2,8-diene skeleton along ...
Claire Cuyamendous+2 more
doaj +2 more sources
3-Bromo-Isoxazoline Derivatives Inhibit GAPDH Enzyme in PDAC Cells Triggering Autophagy and Apoptotic Cell Death [PDF]
A growing interest in the study of aerobic glycolysis as a key pathway for cancer-cell energetic metabolism, favouring tumour progression and invasion, has led to consider GAPDH as an effective drug target to specifically hit cancer cells. In this study,
Bottani, Emanuela+12 more
core +1 more source
Implications of flexible spacer rotational processes on the liquid crystal behavior of 4,5-dihydroisoxazole benzoate dimers [PDF]
The synthesis of some novel non-symmetric liquid crystal dimers, {3-[4-(octyloxyphenyl)]-4,5-dihydroisoxazol-5-yl}alkyl 4-(decyloxy)benzoates (5a–d) and 4-{3-[4-(octyloxyphenyl)]-4,5-dihydroisoxazol-5-yl}alkyl 4-{[6-(octyloxy)naphthalen-2-yl]ethynyl ...
Bechtold, Ivan H.+7 more
core +3 more sources