Results 11 to 20 of about 582 (169)

Spirooxindoles as Disruptors of Preformed Hen Egg White Lysozyme Fibrils as a Model for Neurodegenerative Diseases. [PDF]

open access: yesChemMedChem
Formation of fibrils is a key factor in the development of neurodegenerative diseases. Their highly ordered structure is stabilized by strong hydrogen bonding. Synthesised spirooxindole compounds, Hd‐63, Hd‐66, and Hd‐74, disrupt fibril structure, leading to the breakdown of this order and promoting the formation of off‐pathway aggregates that lack ...
Dahdah A   +3 more
europepmc   +2 more sources

Copper- and Silver-Catalyzed Reactions of Active Methylene Isocyanides: Facile Access to Highly Substituted Five- and Six-Membered Heterocycles. [PDF]

open access: yesChemistry
This review summarizes recent advances in copper‐ and silver‐catalyzed reactions of active methylene isocyanides for the synthesis of highly substituted five‐ and six‐membered heterocycles. Emphasis is placed on [3+n] cycloadditions, annulations, and asymmetric strategies, highlighting current limitations and future opportunities in heterocycle ...
George J, Oh K.
europepmc   +2 more sources

In Vitro and In Silico Evaluation of Isatin-Derived Spirooxindoles as Antituberculosis Drug Candidates. [PDF]

open access: yesChem Biol Drug Des
Two compounds, A16 and A17, were active against multidrug‐resistant Mycobacterium tuberculosis isolates (PT‐12 and PT‐20), overcoming key resistance mutations in katG and rpoB, while cytotoxicity assays confirmed that they are non‐toxic. A17 exhibited the highest antituberculosis activity, with molecular docking suggesting enoyl‐[acyl‐carrier‐protein ...
de Lima FR   +11 more
europepmc   +2 more sources

Deciphering Tryptophan Oxygenation: Key Modulators of 2-Oxindole Formation in MarE. [PDF]

open access: yesAngew Chem Int Ed Engl
This study reveals that MarE, a heme‐dependent aromatic oxygenase, favors dioxygenation of β‐methyl‐l‐tryptophan in the absence of ascorbate and demonstrates how structural and redox tuning shifts its reactivity toward selective monooxygenation, yielding a 2‐oxindole scaffold. These findings offer new insights into enzyme‐controlled indole oxidation in
Nguyen RC, Shin I, Liu A.
europepmc   +3 more sources

Highly diastereoselective cascade [5 + 1] double Michael reaction, a route for the synthesis of spiro(thio)oxindoles

open access: yesScientific Reports, 2021
The first diastereoselective synthesis of spirothiooxindoles is reported via the Michael reaction between thiooxindoles and dibenzalacetones. The reaction was conducted without any catalyst or additive under green conditions, i.e., ethanol as the solvent
Firouz Matloubi Moghaddam   +2 more
doaj   +1 more source

The Solubility Studies and the Complexation Mechanism Investigations of Biologically Active Spiro[cyclopropane-1,3′-oxindoles] with β-Cyclodextrins

open access: yesPharmaceutics, 2023
In this work, we first improved the aqueous solubility of biologically active spiro[cyclopropane-1,3′-oxindoles] (SCOs) via their complexation with different β-cyclodextrins (β-CDs) and proposed a possible mechanism of the complex formation.
Anna A. Kravtsova   +5 more
doaj   +1 more source

Synthesis and Diversification of Chiral Spirooxindoles via Organocatalytic Cascade Reactions

open access: yesChemistry Proceedings, 2023
The synthesis of chiral spirooxindoles through different amino catalytic activation modes is described herein. Several alkenylisatins were obtained from the Knoevenagel reaction of isatin and activated methylene derivatives containing electron ...
Jessica Navarro Vega   +2 more
doaj   +1 more source

3′,4′-Dihydro-2′H-spiro[indoline-3,1′-isoquinolin]-2-ones as potential anti-cancer agents: synthesis and preliminary screening [PDF]

open access: yesRoyal Society Open Science, 2020
Both tetrahydroisoquinolines (THIQs) and oxindoles (OXs) display a broad range of biological activities including anti-cancer activity, and are therefore recognized as two privileged scaffolds in drug discovery. In the present study, 24 3′,4′-dihydro-2′H-
Maloba M. M. Lobe, Simon M. N. Efange
doaj   +1 more source

3′-Methyl-2-oxo-1′,5′-diphenyl-1′,7′-dihydrospiro[indoline-3,4′-pyrazolo[3,4-b]pyridine]-6′-carboxylic Acid

open access: yesMolbank, 2021
3′-methyl-2-oxo-1′,5′-diphenyl-1′,7′-dihydrospiro[indoline-3,4′-pyrazolo[3,4-b]pyridine]-6′-carboxylic acid was synthesized using diverse conditions. The best reaction condition consisted of using water as solvent under microwave irradiation, affording ...
Pablo E. Romo   +3 more
doaj   +1 more source

Synthesis and Characterization of New Spirooxindoles Including Triazole and Benzimidazole Pharmacophores via [3+2] Cycloaddition Reaction: An MEDT Study of the Mechanism and Selectivity

open access: yesMolecules, 2023
A new series of spirooxindoles based on benzimidazole, triazole, and isatin moieties were synthesized via a [3+2] cycloaddition reaction protocol in one step. The single X-ray crystal structure of the intermediate triazole-benzimidazole 4 was solved. The
Saeed Alshahrani   +7 more
doaj   +1 more source

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