A nickel(II) complex with 6-(p-chlorobenzoyl)-5,7,12,14-tetramethyl-benzo[b]-1,4,8,11- tetraazacyclo[14]tetradecine was synthesized and characterized by measurements of NMR, IR and an electronic spectra. The X-ray crystal structure shows that the coordination geometry around the Ni atom is a squ...

Based on the structure of R115777 (tipifarnib, Zarnestra®), a series of farnesyltransferase inhibitors have been synthesized by modification of the 2-quinolinone motif and transposition of the 4-chlorophenyl ring to the imidazole or its replacement by 5-membered rings. This has yielded a novel s...

A series of (1-aryl-1H-pyrazol-4-yl) (3,4,5-trimethoxyphenyl)methanones (8a-p, 9a-p) and ketoxime (10c) derivatives were designed and synthesized as antitubulin agents. All of the target compounds were evaluated for the in vitro anti-proliferative activities against three tumor cell lines (A549,...

The promising anti-Candida agent, 4-chlorophenyl ({[1E-3(1H-imidazole-1-yl)-1-phenylpropylidene}oxy)methanone (4-CPIPM) was comprehensively characterized by FT-IR, FT-Raman, UV, as well as 1H and 13C spectroscopic techniques. The theoretical calculations in the current study utilized Gaussian 09...

The hydrolysis of the p-anisoyl group from the active centre of the thrombolytic proenzyme APSAC has been studied in human plasma, whole blood and thrombin-induced plasma clots using a radiochemical method based on a tritiated acyl group and in human plasma by a fibrinolytic method which exploit...

A convenient synthesis of several ‘phosphomide’ ligands (P adjacent to carbonyl group) from secondary phosphines is reported. The new anisoyl substituted phosphines are considerable more stable to hydrolysis, and are stronger σ-donor ligands than P-acetyl-diphenylphosphine as determined by th...

A series of Gd-doped Li-Ni ferrites with the formula of LiNi0.5GdxFe2-xO4 where x = 0.00 ∼ 0.08 in steps of 0.02, were prepared by thermolysis of oxalate precursors obtained by rheological phase reaction. The structure, morphology, and the magnetic properties of the samples were characterized b...

Diffusion couple experiments for the Mg–Gd and Mg–Y systems were performed with Mg single crystals to investigate the anisotropic diffusion behavior of Gd and Y in hexagonal close packed (hcp) Mg at temperatures between 703 and 803 K (430 and 530 °C). Diffusion coefficients for both Gd and Y ...

A comparison of the primary structures among psychrophilic, mesophilic, and thermophilic subtilases revealed that the turn between the β8 and β9 strands (β8–β9 turn, BPN′ numbering) of psychrophilic subtilases are more flexible than those of their mesophilic and thermophilic counterparts. ...

The fragment of bacterial peptidoglycan muramyl dipeptide (MDP) has long been known for its adjuvant activity, however the underlying mechanism of this action has only recently been elucidated. It is ascribed to its agonist action on the nucleotide-binding oligomerization domain-containing prote...

The Epstein–Barr virus (EBV) nuclear antigen-1 (EBNA1) plays a pivotal role in EBV infection by anchoring the viral episome to cellular DNA, which regulates replication and partitioning in dividing cells. Here, we have used fluorescence recovery after photobleaching (FRAP) and fluorescence loss...

Two cyclic dipeptides, cyclo(His-Ala) and cyclo(His-Gly,) were synthesized from their linear counterparts and their structures elucidated using standard elucidation techniques. Molecular modeling and predictive NMR results indicated that the majority of energetically favourable conformers adopte...

Proton NMR spectroscopy was applied to study the reactions of the dipeptides glycyl-glycine (Gly-Gly) and glycyl-l-alanine (Gly-l-Ala) with hydrogen tetrachloridoaurate(III) (H[AuCl4]). All reactions were performed at pH 2.0 and 3.0 and at 40 °C. The final products in these reactions were [Au(G...

The kinetics of the title reaction has been investigated both in the aqueous and aqueous cationic micelles of tetradecyltrimethylammonium bromide (TTABr) solutions using UV–vis spectrophotometry at 343 K and pH 5.0. Ninhydrin reacts with [Cu(II)–Gly-l-Ala]+ complex in the stoichiometric ratio ...

The conformational space of β-turns of Ala-Gly dipeptide is analyzed theoretically using quantum mechanical methods. A number of potential minima are obtained and characterized. The potential energy surface suggests that β-turn conformers are susceptible to rapid radical formation, which leads...

Many endogenous peptides are circulating in bodily fluids at micromole level, and accurate analysis of endogenous peptides at such low level is important. In this study, we presented an extensible, facile and sensitive sensor array based on UV–Vis spectroscopy of the AuNPs combined with chemome...

SummaryCats pretreated with methiothepin and then injected intramuscularly with a minimum anesthetic dose of ketamine become anesthetized sooner, sleep longer, and take longer to recover than control animals. Instead of muscle tonus and limb rigidity, muscle flaccidity is seen. Limb-withdrawal a...

We previously observed, using in vivo microdialysis, that the potassium-evoked release of frontocortical serotonin (5-HT) is suppressed after rats receive high doses (30 mg/kg, i.p., daily for 3 days) of fluoxetine, a selective, blocker of 5-HT reuptake. We now describe similar impairments in 5-...

SummaryMethiothepin and p-chlorophenylalanine prolong and intensify the initial ataxia and prostration produced by a large intravenous dose (5 mg/kg) of cocaine in dogs. Subsequent behavioral, motor, and toxic effects of cocaine are completely blocked by methiothepin, and completely or partly bl...

Methiothepin has been reported to induce an increase of specific binding sites for 3H-5TH 2–3 days following a single administration of a large dose. The present study was intended to ascertain whether methiothepin pretreatment would induce behavioral serotonergic supersensitivity, as assayed b...