The air-dried fruit hulls of Garcinia mangostana Linn. were extracted with 70% MeOH, and then partitioned into the n-BuOH fractions. Furthermore, three major phenolic components related to their antioxidant activities were purified by silica gel column chromatography and Sephadex LH-20 and then ...
Isothiocyanates (ITCs), a class of phytochemicals with promising cancer-preventive potential, are double-edged swords in the modulation of cellular oxidative stress. While ITCs transcriptionally stimulate many antioxidative enzymes and nonenzyme proteins, leading to enhanced protection against o...
An efficient one-pot synthesis of 3-substituted-5-amino-1,2,4-thiadiazoles from isothiocyanates and amidines is described.
Copper-catalyzed tandem reaction of ortho-bromobenzamides and isothiocyanates is described, which provides an efficient and practical route for the synthesis of 2-thioxo-2,3-dihydroquinazolin-4(1H)-ones. The optimal condition involved the following parameters: CuI as precatalyst, Cs2CO3 as base,...
Base-promoted [3+2] annulation of 2-alkynyl pyrrole with isothiocyanate affording 1H,3H-pyrrolo[1,2-c]thiazol-3-imine derivatives has been developed. The control experiments suggest that the reaction proceeds via simple nucleophilic attack followed by intramolecular addition. The present cascade...
Epidermal growth factor receptor inhibitors (EGFR-TKIs) represent a class of compounds widely used in anticancer therapy. An increasing number of studies reports on combination therapies in which the block of the EGFR-TK activity is associated with inhibition of its downstream pathways, as PI3K-...
An efficient one-pot method for the synthesis of 4-monosubstituted and 4,4-disubstituted 1,4-dihydro-3,1-benzoxazine-2-thiones has been developed. Treatment of 2-bromophenyl isothiocyantes with butyllithium in THF at −78 °C generates 2-lithiophenyl isothiocyanates, which are allowed to react wi...
This study aims to identify the conformational and spectroscopic characteristics of 2,4-xylyl isothiocyanate (C9H9NS) compound via experimental and computational methods. To accomplish this, density functional theory (DFT), with the B3LYP functional was used to determine ground state conformatio...
Plant-parasitic nematodes cause substantial crop losses annually; however, current nematicides are environmentally unfriendly and highly toxic to nontarget organisms. The development of green efficient nematicides from multifunctional natural bioactive substances such as chitin oligosaccharide (...
Four new organotin(IV) ferrocenyl dithiocarbamate complexes viz. [(FcCH2EtOHdtc)2SnR2] (R = Me (1), n-Bu (2) and Ph (3)) and [(FcCH2EtOHdtc)SnPh3] (4) have been synthesized and characterized by electronic absorption, IR, 1H, 13C and 119Sn NMR spectroscopy. The molecular structures of 1 and 2 hav...
The effect of castrix (2-chloro-4-dimethylamino-6-methylpyrimidine) on the distribution of B6 vitamers in mouse brain was determined. The levels of pyridoxal and pyridoxal phosphate decreased, and the levels of pyridoxamine and pyridoxamine phosphate increased at the time of occurrence of convul...
Regioselective displacement reaction of ammonia with 5-bromo-2,4-dichloro-6-methylpyrimidine was studied by X-ray crystallography analysis and showed the formation of 5-bromo-2-chloro-6-methylpyrimidin-4-amine as a main product. Reaction of the latter compound with secondary amines in boiling et...
The solid-state packing arrays of ten 4-chloro substituted 2-aminopyrimidines have been examined and the occurrence of N—H—Cl hydrogen-bonding associations in those structures discussed. The ten compounds were 4,6-dichloropyrimidine 1, 2-amino-4-chloro-6-(4-carbamoylpiperidinyl)pyrimidine hemi...
ObjectivesThe objective of this study was to investigate the use of three new bis-(acrylamide)s as cross-linker in resin-based composite restoratives. Selected mechanical properties such as flexural strength and flexural modulus of model composites containing bis-(acrylamide)s were investigated ...
A substituted 4-aminopiperidine was identified as showing activity in an MCH assay from an HTS effort. Subsequent structural modification of the scaffold led to the identification of a number of active MCH antagonists. 3,5-Dimethoxy-N-(1-(naphthalen-2-ylmethyl)piperidin-4-yl)benzamide (5c) was a...
In a search for novel DPP-IV inhibitors, 2-aminobenzo[a]quinolizines were identified as submicromolar HTS hits. Due to the difficult synthetic access to this compound class, 1,3-disubstituted 4-aminopiperidines were used as model compounds for optimization. The developed synthetic methodology an...
Extrusion of one of the nitrogens of the piperazine ring of potent nootropic drugs previously described gave 4-aminopiperidine analogues that maintained high cognition enhancing activity in the mouse passive avoidance test. One of the new compounds (9, active at 0.01 mg/kg ip) may represent a ne...
A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure–affinity relatio...
We have synthesized a series of C7-piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones that are highly potent inhibitors of both p38 MAP kinase activity and TNF-α release. The 4-aminopentamethylpiperidine naphthyridinone 5, which was designed ...
A two-step sequence involving an Ugi four-component reaction was developed for the preparation of 4-aminopiperidine-4-carboxylic acid derivatives. This strategy has led to the successful preparation of two drugs carfentanil and remifentanil in shorter times and better yields than previously desc...
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