Rh(III)-catalyzed C–H activation of N-(alkyl)benzamides in the oxidative coupling with various quinones. In addition, under redox-neutral conditions, 2-hydroxy-6H-benzo[c]chromen-6-ones were also obtained via a cascade of cross-coupling followed by lactonization.
In present study, a novel series of fluorine containing 4-(2-pyrimidinylamino)benzamide analogues were designed and synthesized. The hedgehog (Hh) signaling inhibitory activities for these compounds were evaluated by a luciferase reporter method. The preliminary SAR was discussed and many compou...
Five 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives of lupinine, epi-lupinine and lupinylamine, together with two 1-homolupinanoyl benzimidazolones were prepared and investigated for their ability to displace specific radioligands from 5-HT3 and 5-HT4 receptors. The synthesized...
A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure–activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the SAR associated with an X-ray structure of on...
We report here the synthesis and preliminary evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives 6(a–k) and their precursors 5(a–k) as potential chemotherapeutic agents. In each case, the structures of the compounds were determined by FTIR, 1H NMR and mass...
In an attempt to find a potent inhibitor of antileukaemic activity, we performed two-dimensional quantitative structure–activity relationship studies. The QSAR models of the 1-(4-methoxyphenethyl)-1H-benzimidazole derivatives were developed by means of utilizing simulated annealing for the purp...
Publisher SummaryThis chapter describes the synthesis, characterization, and analysis of dicarboxylylmono–coenzyme A esters by reversed-phase high-performance liquid chromatography (HPLC) and illustrates the application of these methods to studies of the intermediates of [U-14C]hexadecanedioylm...
The asymmetric ring opening reaction of 1,2-(N-acylimino)cyclohexanes (N-acylaziridines) with some thiols proceeded in the presence of chiral zinc complexes prepared from diethylzinc and dialkyl L-(+)-tartrate to afford trans 2-(N-acylamino)-1-arylthiocyclohexane in up to 93% ee. The enantiosele...
Optically active tartaric acid and its diester derivatives are well known as effective chiral selectors. In the current studies, a self-prepared diester of tartaric acid (2R, 3R)-di-n-propyl tartrate (DPT) was used as a chiral mobile-phase additive (CMPA) for the enantioseparation of seven kinds...
A chromatographic method for the determination of the enantiomeric purity of (S)-atropine is presented and has been applied to the analysis of tablets. The (2S,3S)-enantiomer of the chiral selector, dicyclohexyl tartrate, was used as selector in order to elute the impurity, (R)-atropine, before ...
The enantiomers of acids, esters and amino alcohols of moderate hydrophobicity containing two hydrogen bonding functions were separated in underivatized form using (2R,3R)-dicyclohexyl tartrate (DCHT) in phosphate buffer (pH 3) as mobile phase and porous graphitic carbon (Hypercarb) as stationar...
PurposeThe effect of chronic administration of [3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate (URB597), inhibitor of fatty acid amide hydrolase (FAAH) that hydrolyzes anandamide, on cross-talk between endocannabinoid system, oxidative status and pro-inflammatory factors in the liver of spon...
The bioactive substance investigation of Balanophora involucrata obtained 15 phenolic acids, including 5 new compounds (1–3, 8, 9), which were determined by various spectroscopic data analyses. Most isolated compounds displayed inhibitory effects on α-Glucosidase in vitro. For the potential in...
Single enantiomer cyclopropylalanine (>99.9% ee) and various derivatives were prepared using an asymmetric hydrogenation approach with a rhodium catalyst based on the methyl BoPhoz™ ligand. N-Boc cyclopropylalanine benzyl ester was the preferred derivative, as this material is ripe for further s...
Residualizing radioactive labels are designed to remain entrapped within cells following degradation of a carrier protein, and have been used for identification of the tissue and cellular sites of plasma protein catabolism. In this study we describe a convenient synthesis and purification of a s...
A biologically active 125I-substance P derivative (I125-BH-substance P), prepared by conjugation of substance P with [125I]Bolton-Hunter reagent, binds specifically to isolated rat parotid cells. The Kd is 4 nM for I-BH-substance P, 5 nM for substance P, 0.18 μM for substance P octa(4–11)pepti...
Problems in interpretation of autoradiograms generated by ligand binding in brain tissue may be caused by two types of technical limitations: the differential absorption of3H-generated emissions within the tissue (differential quenching) and the reduced resolution when125I and14C are used as iso...
The biodistribution has been assessed in mice of synthetic branched polypeptides. These were: A poly(l-lysine) backbone with short side chains of three dl-alanine residues (AK, which is polycationic); AK with an additional glutamic acid residue at the end of the branches (EAK, which is amphoteri...
Publisher SummaryThis chapter describes procedures for labeling human interferon (Hu-IFN)-α with 125I-labeled Bolton–Hunter reagent and the purification of the radiolabeled ligand. Radioactive derivatives of IFN have been prepared by several iodination procedures, which chemically add a radioa...
Radioiodinated 2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane, 5 (4-HIPP), was synthesized and evaluated as a simple vesamicol-like radiotracer for mapping cholinergic pathways in the brain. Both enantiomers of 5 exhibit significant accumulation (approx. 2% of injected dose) and prolo...
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