AI Article Synopsis

  • Bifunctional building blocks, like aryl glyoxal, have significant importance in synthetic chemistry due to their versatile applications.
  • Aryl glyoxal is particularly valuable in creating various five- and six-membered heterocycles, which are essential components of many natural products.
  • Recent advancements highlight the use of multicomponent reactions with aryl glyoxal to efficiently synthesize diverse oxygen heterocycles.

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Neurodegenerative diseases (NDs) are one of the prominent health challenges facing contemporary society, and many efforts have been made to overcome and (or) control it. In this research paper, we described a practical one-pot two-step three-component reaction between 3,4-dihydronaphthalen-1(2)-one (), aryl(or heteroaryl)glyoxal monohydrates (-), and hydrazine monohydrate (NHNH•HO) for the regioselective preparation of some 3-aryl(or heteroaryl)-5,6-dihydrobenzo[]cinnoline derivatives (-). After synthesis and characterization of the mentioned cinnolines (-), the multi-targeting inhibitory properties of these heterocyclic scaffolds have been investigated upon various -type enzymes, including MAO-A, MAO-B, AChE, BChE, BACE-1, BACE-2, NQO-1, NQO-2, nNOS, iNOS, PARP-1, PARP-2, LRRK-2, GSK-3β, p38α MAPK, JNK-3, OGA, NMDA receptor, nSMase-2, IDO-1, COMT, LIMK-1, LIMK-2, RIPK-1, UCH-L1, PARK-7, and DHODH, which have confirmed their functions and roles in the neurodegenerative diseases (NDs), based on molecular docking studies, and the obtained results were compared with a wide range of approved drugs and well-known (with IC, EC, etc.

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Article Synopsis
  • The text discusses innovative, environmentally friendly methods for synthesizing hybrid medicinal compounds that contain multiple bioactive components without using metals or toxic chemicals.
  • It details a specific reaction that occurs at room temperature, utilizing a unique solvent and resulting in the formation of various hybrid molecules, specifically pyrazole-linked thiazoles and barbiturates.
  • The advantages of this method include simple operation, high efficiency, minimal waste (water as a byproduct), and the ability to produce substantial amounts of the desired compounds.
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Glyoxal oxidases, belonging to the group of copper radical oxidases (CROs), oxidize aldehydes to carboxylic acids, while reducing O to HO. Their activity on furan derivatives like 5-hydroxymethylfurfural (HMF) makes these enzymes promising biocatalysts for the environmentally friendly synthesis of the bioplastics precursor 2,5-furandicarboxylic acid (FDCA). However, glyoxal oxidases suffer from inactivation, which requires the identification of suitable redox activators for efficient substrate conversion.

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Glyoxalase-based toolbox for the enantioselective synthesis of α-hydroxy carboxylic acids.

Org Biomol Chem

March 2024

Department of Chemistry, School of Sciences and Humanities, Nazarbayev University, 53 Kabanbay Batyr Ave, Astana, 010000, Kazakhstan.

We report highly enantioselective synthesis of L-α-hydroxy carboxylic acids (L-αHCAs) enzymatic intramolecular Cannizzaro reaction of (hetero)aryl glyoxals in the presence of glutathione-independent human glyoxalase DJ-1. Combined with the optimized synthesis of D-αHCAs using glyoxalases I and II, this approach offers a general, scalable and operationally simple access to both enantiomers of α-hydroxy acids in moderate to excellent yields with uniformly high enantioselectivity.

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In the research, the core-shell procedure synthesized a novel magnetically separable heterogeneous nanocatalyst with high stability named FeO@CPTMO@dithizone-Ni. In this method, FeO was modified as a magnetic core using surfactant (SDS) and polyethylene glycol (PEG) coating; after functionalizing the magnetic nanoparticles with 3-chloropropyl-tri-methoxysilane and dithizone, Ni metal was immobilized. The prepared catalyst was identified and specified utilizing diverse physicochemical techniques involving FT-IR, XRD, SEM, EMA, BET, ICP, EDS, TGA, Raman, and TEM.

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