Recently [11C]mG4P012 (previously [11C]KALB012 and presently named as [11C]PXT012253 by Prexton Therapeutics) had been used as a biomarker during the preclinical development of a potential therapeutic drug, PXT0002331 (an mGluR4 PAM), for PD and l-dopa-induced dyskinesia. [11C]mG4P012 was shown ...
The molecular and crystal structures of the title compound have been determined from a single crystal neutron diffraction experiment at 100 K. A comparison between the main geometrical features and related properties of the in-crystal and the ab initio optimized free molecule structures has show...
Electrochemical oxidation of 3,4-dihydroxybenzoic acid (1a) has been studied in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as a nucleophile in aqueous solution using cyclic voltammetry and controlled-potential coulometry. The results indicate that 1a via a 1,4-(Michael) addition reac...
Electrochemical oxidation of o-dihydroxybenzenes (1a and 1b) has been studied in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as a nucleophile in aqueous solution using cyclic voltammetry and controlled-potential coulometry. The results indicate that the o-quinones derived from o-dihyd...
Electrochemical oxidation of catechols (1a–1c) has been studied in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as a nucleophile in aqueous solution using cyclic voltammetry and controlled-potential coulometry. The results indicate that the quinones derived from catechols (1a–1c) par...
We report here the synthesis of aromatic coumarins and aromatic α-quinolones which were evaluated in vitro for their protective potentialities against tert-butyl hydroperoxide (t-BHP)-induced oxidative damage on human liver cell death, i.e., human hepatoma HepG2 cell line and human hepatocytes ...
Synthesis of some novel hetarylazoquinoline dyes was achieved by diazotisation of nine heterocyclic amines using nitrosyl sulphuric acid, coupling with 2,4-quinolinediol. These dyes were characterized by UV–vis, FT-IR and 1H NMR spectroscopic techniques and elemental analysis. Visible absorptio...
A series of 1,1′-bis[N-formyl-N′-substituted thiourea]ferrocene derivatives was synthesized through the reaction of 1, 1′-bis[formyl isothiocyanate]ferrocene and various primary amines, with high yields after simple and convenient purification. All the compounds were characterized by elementa...
A series of new synthesized N-bis(trifluoromethyl)alkyl-N’-substituted ureas have been tested in the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10−5 M). COMPARE analysis has been carried out for all tested compounds. ...
C2-Symmetric normal and mesoionic bis-N-heterocyclic carbenes (NHCs) derived from 1,1′-((1,1′-biphenyl)-2,2′-diylbis(methylene))bis(3-methyl-4-phenyl-1H-1,2,3-triazol-3-ium) diiodide (5) and 3,3′-((1,1′-biphenyl)-2,2′-diylbis(methylene))bis(1-phenyl-1H-imidazol-3-ium) dibromide (6) were us...
Five halo-containing chitosan 3,6‑bis(phenylcarbamate)‑2‑(cyclobutylformamide) derivatives were synthesized with well-deacetylated chitosan and halo-substituted phenyl isocyanates. The structures of the derivatives were characterized by IR, elemental analysis, and 1H NMR spectrum. After being co...
The Kabachnik–Fields condensation was extended using secondary phosphine oxides, such as dibenzylphosphine oxide and bis(4-methylphenyl)phosphine oxide as the P-reactant in reaction with formaldehyde and different primary amines. Besides the α-aminophosphine oxides, the corresponding bisproduc...
Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal p...
The Schiff base compound, N,N′-bis(trifluoromethylbenzylidene)ethylenediamine (C18H14F6N2) (1), CF3C6H4CHNCH2CH2NCHC6H4CF3 has been synthesized by adding a solution of ethylenediammine (en), 0.1 mmol in chloroform to 4-(trifluoromethyl)-benzaldehyde, CF3C6H4CHO (0.2 mmol) and the product was cr...
A rapid and simple spectrophotometric method was developed for the determination of copper(II) by using newly synthesized chromogenic reagent, N″,N″′-bis[(E)-(4-fluorophenyl)methylidene]thiocarbonohydrazide [bis(4-fluoroPM)TCH]. The reagent is highly sensitive and it forms yellow colored tern...
Benzothiazolyl thiocarbamides has been achieved using a catalytic amount of 4-dimethylaminopyridine (DMAP) followed by its chemoselective oxidative cyclization with 1,3-di-n-butylimidazolium tribromide[bbim][Br3] to afford the N-bis-benzothiazole derivatives. All the synthesized compounds were e...
Reaction of N,N-dimethylaniline, N,N-dimethylnaphthalen-1-amine and 1,8-bis(dimethylamino)naphthalene (proton sponge) with 1-chloromethyl-4-fluorodiazonia-bicyclo[2.2.2]octane bis(tetrafluoroborate) (Selectfluor) and N-fluorobenzenesulfonimide (NFSI) has been studied under various conditions. Un...
New homoleptic nickel(II) biscarbene complex was synthesized and structurally characterized. The complex depicted the excellent catalytic activities with only 3 mol% catalyst loading along with wide substrate scope for the Suzuki–Miyaura cross-coupling reactions (twenty six examples) and Heck c...
Hydrodisulfides (RSSH) have previously been implicated as key intermediates in thiol-triggered oxidative DNA damage by the antitumor agent leinamycin. In an effort to better understand DNA damage by RSSH and to expand on the number and type of chemical systems that produce this reactive intermed...
3,1-Benzoxathian-4-ones, 2, when heated with 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane-2, 4-disulfide, 1, or with P4S10 give one or more of the following products 3,1-benzoxathian-4-thione, 3, 1,3-benzodithian-4-one, 4, 1,3-benzodithian-4-thione, 5, and 3H-1,2-benzodithiole-3-thione, ...
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