Synergistische Entwicklungsstrategien von Inhibitoren gegen humane UDP‐Galactose‐4‐Epimerase
Die Epimerase GalE ist essenziell für die Biosynthese von krebsrelevanten O‐GalNAc Glykanen. Wir verwenden orthogonales, strukturbasiertes Screening niedermolekularer Fragmente an, um kovalente und nichtkovalente Inhibitoren gegen GalE mit nicht mehr als 22 optimierten Verbindungen zu erhalten.
William M. Browne +22 more
wiley +1 more source
Nitroimidazoles XIII. Synthesis of Substituted (1-Methyl-5-Nitro-2-Imidazolyl) Isoxazoles [PDF]
The beta0diketone derivatives of nitroimidazole were synthesized from the reaction of magnesium salt of beta-ketoaccids 3 with imidazolide 4. The raction of beta-diketones with hydroxylamine hydrochloride afforded either the isoxazoles or the 5-hydroxyl ...
Abbas Shafiee, Mohammad ALi Ebrahimzadeh
doaj
Deep Eutectic Solvents: The Organic Reaction Medium of the Century [PDF]
This microreview summarizes the use of deep eutectic solvents (DESs) and related melts in organic synthesis. Solvents of this type combine the great advantages of other proposed environmentally benign alternative solvents, such as low toxicity, high ...
Abbott +192 more
core +2 more sources
Electrochemical Synthesis of Isoxazoles and Isoxazolines via Anodic Oxidation of Oximes
Isoxazol(in)es are widely featured structural motifs in natural products, agrochemicals, and pharmaceuticals. The first intermolecular approach for a direct electrochemical synthesis from readily available aldoximes is reported.
Silja Hofmann +4 more
doaj +1 more source
A low-toxicity method for the separation of lanosterol and dihydrolanosterol from commercial mixtures [PDF]
We describe an inexpensive, low-toxicity and high-yielding method for the production of pure lanosterol and dihydrolanosterol from the commercially available mixture.
Kavtaradze, Levan K. +2 more
core +2 more sources
A Synergistic Inhibitor Development Strategy Against Human UDP‐Galactose‐4‐Epimerase
The epimerase GalE is crucial for the biosynthesis of cancer‐relevant O‐GalNAc glycans. Here, we employ orthogonal, structurally enabled small molecule fragment screens to yield both covalent and non‐covalent inhibitors against GalE within no more than 22 elaborated compounds.
William M. Browne +22 more
wiley +1 more source
5-(Benzoyloxymethyl)isoxazole-3-carboxylic Acid Ethyl Ester
We describe here the palladium hydrogenation of ethyl 5-(benzoyloxymethyl)isoxazole-3-carboxylate. The presence of two reducible sites in the molecule, namely the benzylic-like position and the isoxazole N–O bond, creates a possible competition.
Cosimo Antonini +2 more
doaj +1 more source
Synthesis and biological evaluation of ferrocene-based cannabinoid receptor 2 ligands [PDF]
Ferrocene analogues of known fatty acid amide hydrolase inhibitors and CB2 ligands have been synthesized and characterized spectroscopically and crystallographically.
Barczyk, Amélie +11 more
core +3 more sources
Síntesis y evaluación “in vitro” de la actividad antifúngica de oximas, éteres de oxima e isoxazoles
Synthesis and in vitro assessment of antifungal activity of oximes, oxime ethers and isoxazoles. Objective. To synthesize and carryout a preliminary evaluation of the in vitro antifungal activity of oximes, oxime ethers and isoxazoles.
John Diaz-Velandia +3 more
doaj
Tolerância de híbridos de milho ao herbicida isoxaflutole Tolerance of corn hybrids to isoxaflutole
Objetivou-se com este trabalho avaliar a tolerância de híbridos de milho ao isoxaflutole e relacionar estudos de seletividade desse herbicida conduzidos em casa de vegetação com estudos desenvolvidos em campo.
S.D. Cavalieri +5 more
doaj +1 more source

