A5103096208- Chemical synthesis and alkaloids
- Cholinesterase and Neurodegenerative Diseases
- Nicotinic Acetylcholine Receptors Study
- Synthesis and Biological Evaluation
- Chemical Reaction Mechanisms
- Multicomponent Synthesis of Heterocycles
- Asymmetric Synthesis and Catalysis
- Conservation Techniques and Studies
- Chemical Synthesis and Analysis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and biological activity
- Cultural Heritage Materials Analysis
- Synthesis and Reactions of Organic Compounds
- Computational Drug Discovery Methods
- Synthesis of heterocyclic compounds
- Building materials and conservation
- Melanoma and MAPK Pathways
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Radical Photochemical Reactions
- Synthesis and Characterization of Heterocyclic Compounds
- bioluminescence and chemiluminescence research
- Catalytic C–H Functionalization Methods
- Peptidase Inhibition and Analysis
- Receptor Mechanisms and Signaling
- Dental materials and restorations
Queen Mary University of London
2024
Centro de Investigación en Materiales Avanzados
2024
Deutsches Bergbau-Museum Bochum
2021-2022
Universidad Autónoma de Madrid
2004-2021
Universität Trier
2021
Helwan University
2021
Badr University in Cairo
2021
Universidad Complutense de Madrid
2021
Universidad Europea
2021
University of Alicante
2021
Two isomeric series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their ability to inhibit AChE, butyrylcholinesterase, AChE-induced self-induced β-amyloid (Aβ) aggregation, β-secretase (BACE-1) cross blood−brain barrier. The new hybrids consist a unit 6-chlorotacrine multicomponent reaction-derived pyrano[3,2-c]quinoline scaffold as the active-site peripheral-site interacting moieties, respectively, connected through an...
The interaction of cyclic enol esters with diversely substituted anilines and ethyl glyoxalate yields, under Sc(OTf)3 catalysis, disubstituted N-aryl lactams in a multicomponent reaction. protocol allows access to the trans stereoisomers after an epimerization initial mixture which cis isomers predominate. Vinyl acetate yields quinoline derivatives, whereas isopropenyl leads corresponding Mannich adducts.
Double agent: The insertion of two isocyanide molecules into the dihydropyridine ring in presence iodine results formation a benzimidazole core (see scheme). Four bonds are generated (bold lines) highly efficient and atom-economical manner. Access to range benzimidazolium derivatives is possible through cascade reaction.
Janus kinases (JAKs) have a key role in regulating the expression and function of relevant inflammatory cytokines involved asthma chronic obstructive pulmonary disease. Herein are described design, synthesis, pharmacological evaluation series novel purinone JAK inhibitors with profiles suitable for inhaled administration. Replacement imidazopyridine hinge binding motif present initial compounds this pyridone ring resulted mitigation cell cytotoxicity. Further systematic structure–activity...
Two 12-amino-6,7,8,11-tetrahydro-7,11-methanocycloocta[b]quinoline derivatives [9-Me(Et)] (syn-huprines) have been obtained by condensation of known 7-alkylbicyclo[3.3.1]non-6-en-3-ones with 2-(trifluoromethyl)aniline, followed basic cyclization the resulting imine, and chromatographic separation regioisomeric mixture products, thus obtained. The new (±)-syn-huprines were shown to be slightly less active bovine or human acetylcholinesterase inhibitors than corresponding anti-derivatives....
Identifying the most vulnerable plastics and monitoring their deterioration is one of main problems within heritage collections with historical synthetic polymers. Gathering interpreting data about material degradation phenomena in a collection reveals its conservation needs. A systematic survey can help towards this purpose. Surveys aiming at inspecting documenting damages rely on several tools order to fulfill Firstly, objective descriptions that may appear, secondly, means acquiring...
This study compared the initial and one year shear bond strengths (SBS) of resin composite bonded to amalgam using Amalgambond-Plus.Resin cylinders (Point 4, Kerr Corporation) were either etched-enamel (A), 50% etched enamel-50% polished (B), airborne-particle abraded (C), carbide bur prepared (D) amalgam-50% (E). Shear determined a standardized testing device (Ultradent Products) in universal machine (Instron model 4204). The failed interfaces evaluated with SEM obtain visual evidence...
We have studied the base-promoted heterocyclization of alkyl N-(cis(trans)-3,trans(cis)-4-dibromocyclohex-1-yl)carbamates and N-(cis(trans)-3,trans(cis)-4-dibromocyclohex-1-yl)-2,2,2-trifluoroacetamides, investigating effect nitrogen protecting group relative configuration leaving at C3 C4 on outcome this reaction. observed that sodium hydride-promoted N-(cis-3,trans-4-dibromocyclohex-1-yl)carbamates (10, 12, 14, 16, 18) is a convenient method for synthesis 7-azabicyclo[2.2.1]heptane...
Prolyl oligopeptidase (POP) is a cytosolic serine peptidase that hydrolyzes proline-containing peptides at the carboxy terminus of proline residues. This has gained importance as target for treatment cognitive disturbances patients with neuropsychiatric diseases. Our research addresses identification POP inhibitors from small focused library polar heterocyclic compounds arising multicomponent reactions. Two selective POP-specific were identified on basis their inhibition dipeptidyl IV. The...
Abstract The interaction of electrophilic reagents (sulphonic acids, halogens and phenylselenyl chloride) with dihydropyridines cyclic enol ethers generates reactive cationic intermediates which interact isocyanides to afford α‐carbamoylated (β‐substituted) heterocycles after aqueous quenching, in Ugi‐ Passerini‐type reactions. Some post‐condensation transformations (elimination nucleophilic substitution reactions) on these compounds further expand the synthetic scope processes.
The synthesis of 2-substituted 5-amino-4-cyano-1,3-oxazoles (1-4, 6-11) and the Friedländer-type reaction compounds 1, 3, 4 is described.Compounds 13-17 are tacrine (18) analogues provided by Friedländer reaction.The anti-cholinesterase activity 13, 14, 16 17 has been investigated.
The acetylcholinesterase (AChE) inhibitory activity of a series 13-amido derivatives huprine Y, designed to enlarge the occupancy catalytic binding site by mimicking piridone moiety present in (−)-huperzine A, has been assessed. Although both 13-formamido and 13-methanesulfonamido are more potent human AChE inhibitors than tacrine none them equals potency Y. Molecular modeling studies show that two effectively trigger Gly117-Gly118 conformational flip induced upon leading similar pattern...
Doppelter Einsatz: Die Insertion von zwei Isocyanidmolekülen in einen Dihydropyridinring führt Gegenwart Iod zu einer Benzimidazoleinheit (siehe Schema). Dabei werden auf hoch effiziente und atomökonomische Weise vier Bindungen geknüpft (dicke schwarze Linien). Eine Reaktionskaskade eröffnet Zugang vielfältigen Benzimidazolium-Derivaten. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2001/2007/z605070_s.pdf or from author. Please...