Results 81 to 90 of about 5,265 (218)
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
Push–Pull Ynamines and Push–Pull Ynamides: Synthesis, Structure, Reactivity, and Application
Push–pull ynamines and push–pull ynamides, which carry an EWG and an amino or amido group as EDG, are highly interesting classes of EDG‐EWG alkynes that have been intensively studied due to their exceptional reactivity. In this review, the synthesis, structure, reactivity, and application of push–pull ynamines, push–pull ynecarbamates, push–pull ...
Hans‐Joachim Gais
wiley +1 more source
Silver-Catalyzed Synthesis of Disubstituted Fluorinated Isoxazoles
The presence of fluorine can provide organic compounds with useful biological properties, such as increased metabolic stability and drug uptake. Because of these advantages, fluorinated compounds make up about 30% of the drug industry.
Stewart, Micah
core
Calcium-mediated one-pot preparation of isoxazoles with deuterium incorporation
In this work, a novel synthetic methodology for the one-pot preparation of isoxazoles directly from the reaction of calcium carbide with aldoximes is reported.
Konstantin S. Rodygin +2 more
core +1 more source
An efficient, scalable, and versatile base‐triggered synthesis of sulfur‐substituted imides with the utility of alkyl isothiouronium salts and masked carboxylic acids under mild reaction conditions. Imides have a vast presence in pharmaceuticals and natural products, and their synthesis generally relies on the utility of the disagreeable strong ...
Malibongwe P. Shandu +4 more
wiley +1 more source
Copper(0) Nanoparticles in Click Chemistry: Synthesis of 3,5-Disubstituted Isoxazoles
An efficient procedure for the synthesis of 3,5-disubstituted isoxazoles via 3+2 cycloaddition reaction of in situ generated nitrile oxides with acetylenes employing readily preparable copper(0) nanoparticles is described.
Vishwanatha, T.M., Sureshbabu, V.V.
core +1 more source
Synthetic isoxazole as antiplatelet agent
Abstract Nine synthetic isoxazoles were evaluated as antiplatelet agents and studied the possible mechanism of more active compound. The initial screening was evaluating all compounds against platelet aggregation assays. The most active compound was isoxazole 8 showing an inhibition of platelet aggregation around 70%. In subsequent experiments, ADP and
Gutierrez, Margarita +4 more
openaire +4 more sources
Reaction of enantiopure 3,4-dialkoxy-pyrroline N-oxides with benzyne affords the expected tetrahydrobenzo[d]pyrrolo[1,2-b]isoxazoles along with an unexpected 2,3-disubstitued-N-phenyl-pyrrole derived from an unprecedented rearrangement of the adduct of ...
Franca M. Cordero +3 more
doaj +1 more source
The synthesis and reactivity of α-oxoketenes dithioacetals (S,S-acetals), general structure [(R¹C=OC(R²)=C(SR³)(SR4)], are reported. We also showed the application of S,S acetals as synthons for efficient synthesis of isoxazoles, pyrazoles ...
Geonir M. Siqueira +5 more
doaj +1 more source
Versatile and Efficient Solid-Phase Syntheses of Pyrazoles and Isoxazoles
Condensation of aromatic or aliphatic esters with resin-supported acetyl carboxylic acids 2, followed by cyclization with hydrazines or hydroxylamine, activation of the linker, and cleavage using amines provides highly substituted, isomeric pyrazoles or ...
Min Shu (261988) +2 more
core +1 more source

