Metabotropic glutamate receptor 5 (mGlu5) is a biological target implicated in major neurological and psychiatric disorders. In the present study, we have investigated structural determinants of the interaction of negative allosteric modulators (NAMs) with the seven-transmembrane (7TM) domain of...
Vilsmeier–Haack reaction of β-ketoaldehydes leads to the formation of β-chloroenones and these chloroenones on treatment with malononitrile afford 2-hydroxy-5,6-diarylnicotinonitriles. But a one-pot reaction of β-ketoaldehydes with Vilsmeier–Haack reagent and malononitrile or cyanoacetamide...
Using anthraquinone 2-yl ethyl (Aqe) as a photolabile protecting group for carboxylic acids, five caged compounds, Aqe esters of p-methoxybenzoic acid (1a), o-methylbenzoic acid (1b), benzoic acid (1c), p-nitrobenzoic acid (1d) and N-acetyl-l-tryptophan (1e), have been prepared, and their photoc...
Silylated functionalized arylboronic acids were converted into corresponding iodinated arylboronic acids in good yields via the electrophilic ipso-desilylation effected with iodine chloride in refluxing CHCl3. Disilylated arylboronic acids were susceptible to diiodination. In addition, the struc...
By means of “1,2,4-triazine” strategy new 2,2′-bipyridine-type lanthanide ligands, i.e. 5-aryl-2,2′-bipyridine-6′-carboxylic acids and its cycloalkane-annulated derivatives, i.e. 6-(4-aryl-6,7-dihydro-5H-cyclopenta[c]pyridin-1-yl)picolinic acids, have been synthesized, and their luminescent...
An efficient catalytic system has been developed for the synthesis of unsymmetrical substituted alkynes via the thiosemicarbazone salicylaldiminato palladium(II)-catalyzed alkynylation couplings between arylboronic acids and alkynes or alkynyl carboxylic acids under mild conditions.
(4R-trans)-2-(1-Methylethenyl)-1,3,2-dioxaborolane-4,5-dicarboxylic acid, bis- ethyl ester upon oxidation with trimethylamine oxide gives a chiral enol borate that condenses with aldehydes to give optically active 4-hydroxy-2-alkanones in 55-77% yield and 41-65% e.e.
In this investigation, we searched for novel MAO-A inhibitors using a 3-benzylquinoxaline scaffold based on our earlier findings. Series of N′-(3-benzylquinoxalin-2-yl)acetohydrazide, 4a, N′-(3-benzylquinoxalin-2-yl)benzohydrazide derivatives 4b–f, N′-[2-(3-benzyl-2-oxoquinoxalin-1(2H)-yl)ac...
The subcellular distribution and acetylation of the choline analogue, N, N,N-trimethyl-N-3-hydroxypropylamine (homocholine) was studied using the electromotor system of Torpedo marmorata. Both choline and homocholine were transported into nerve terminals by the same high-affinity uptake mechanis...
Laccase (LAC) belongs to the blue multi‑copper lignolytic oxidase enzymes, and has been regarded as an important tool to produce some important dimers in the application of biotechnology. In this study, sixteen coumarins 1–16 were screened to investigate the catalytic ability of LAC, and three ...
Enthalpy and vapour-liquid equilibrium (VLE) characteristics of CO2 absorption in aqueous solution of a new polyamine, bis(3-aminopropyl) amine known as dipropylenetriamine (DPTA) and its aqueous mixture with monoethanolamine (MEA), N-methyldiethanolamine (MDEA), 2-amino-2-methyl-1-propanol (AMP...
In order to prepare 3-aminopropyl glycosides of Neu5Ac-α-(2→6′)-lactosamine trisaccharide 1, and its N-glycolyl containing analogue Neu5Gc-α-(2→6′)-lactosamine 2, a series of lactosamine acceptors with two, three, and four free OH groups in the galactose residue was studied in glycosylatio...
(±)-3-(2-Aminopropyl)-7-benzyloxyindole 1, assembled from 7-benzyloxyindole 3 in 59% overall yield, is resolved with O,O′-di-p-toluoyl l-(2R,3R)-tartaric acid 7 into (R)-1, a key intermediate of AJ-9677 2 (selective adrenaline β3-agonist) in 99.5% e.e. and 36% overall yield. The unwanted enan...
Designing novel catalytic system for efficient synthesis of enantiomerically pure β-hydroxy nitroalkanes is a challenging area of research. Herein, we have designed a chiral heterogeneous catalyst through the successful loading of chiral Cr(III)-salen complex over sulfonic acid functionalized S...
Bimetallic carboxylates of Rh(II) are widely recognized for their ability to catalyze carbene transfer reactions such as the cyclopropanation of olefins using organic diazo compounds as carbene precursors. A major goal in catalysis is to find cheaper, more Earth-abundant alternatives to precious...
Polyhedral oligomeric silsesquioxanes (POSSs) were attached to conventional bis(diphenylphosphino)amine (PNP) ligand as solubility-enhancing materials for catalytic ethylene trimerization and tetramerization. Differently functionalized arylphosphine ligands of the type (Ph)2PN(POSS)P(Ph)(ArR) (R...
A series of new half-sandwich chromium(III) complexes Cp′[2-R1-6-(CHNR2)C6H2O]CrCl [R1 = iPr (1), tBu (2, 3, 4, 5); R2 = iPr (2, 4, 5), tBu (1, 3); Cp′ = C5H5(1, 2, 3), C5H2Ph3 (4), C5Me4Ph(5)] were synthesized from the reactions of Cp′CrCl2(THF) with corresponding salicyladiminato lithium. A...
5-Hydroxymethylfurfural is an important bio-based chemical that shows broad application potential. In the present study, the use of chitosan nanoparticles was proposed to adsorb and recycle chromium ions from aqueous solution with Cr(III) and Cr(VI) removal rates of up to 97.5% and 81.2%, respec...
A combined quantum chemistry and electrochemistry study of a series of tris(β-diketonato)-Cr(III) complexes showed that the different electron donating properties of the R and R' groups, substituted on the 1 and 3 positions of the β-diketonate ligand (RCOCHCOR')−, largely influence t...
Supplements containing chromium in its trivalent oxidation state [Cr(III)] are used by diabetic patients to improve their glucose and insulin levels and omega-3 fatty acids are also beneficial for people with insulin resistance or diabetes. It seemed very useful to combine chromium(III) and omeg...
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