Four copper(II) complexes (1–4) and a cobalt(II) complex (5) derived from 4-bromo-2-(hydroxymethyl)pyridine (L1) or 5-bromo-2-hydroxymethyl)pyridine (L2) with Cu(NO3)2·3H2O, CuCl2·2H2O and CoCl2·6H2O have been synthesized and their respective crystal structures studied. They show specific in...

Comprehensive theoretical and experimental FTIR and FT-Raman spectroscopic studies of 2-(hydroxymethyl)pyridine (2HMP) and 3-(hydroxymethyl)pyridine (3HMP) have been carried out by using DFT/B3LYP method with 6-311++G**, 6-31G** and cc-pVTZ basis sets. The most stable geometry of the compounds h...

This paper describes firstly an effective protocol for the synthesis of a new series of five examples of 3-(trifluoromethyl)-3,3a-dihydrospiro[chromeno[4,3-c]isoxazole-4,1′-cycloalkan]-3-ols (4), in which the cycloalkanes — cyclopentane, cyclohexane, cycloheptane, and 4′-methyl- and 4′-t-but...

A sensitive LC–MS method was developed and validated for the determination of niflumic acid (NFA), the active metabolite of the talniflumate formulation, in human plasma. The analyses were performed on C18 column using acetonitrile–ammonium acetate buffer (pH 5.7, 40:60) as a mobile phase with...

Interest in submicron-sized drug particles has emerged from both laboratory and industrial perspectives in the last decade. Production of crystals in the nano size scale offers a novel way to particles for drug formulation solving formulation problems of drugs with low solubility in class II of ...

The aim of this study was to assess whether nanofibrous drug mats have potential as delivery systems for poorly water-soluble drugs. Amorphous nanofiber mats from a model poorly water-soluble active pharmaceutical ingredient (API), niflumic acid, together with the polymer excipient, polyvinyl py...

New organic ligand L (1) resulting from isonicotinic hydrazide and 2,4-pentanedione has been prepared and investigated by physicochemical methods, including elemental analysis, 1H and 13C NMR, IR spectroscopy and X-ray studies.The X-ray investigation revealed that the condensation of 2,4-pentane...

Nicotinic and isonicotinic thiosemicarbazide or hydrazine carbothioamides 3–27 were synthesized and the structures of synthetic compounds were elucidated by various spectroscopic techniques such as EI-MS, 1H-, and 13C NMR. Synthetic derivatives were evaluated for their urease inhibitory activit...

Molecular imprinting of nicotine was performed using an acidic functional monomer 2-(trifluoromethyl)acrylic acid (TFMAA). Chromatographic studies using the resultant polymers as stationary phases displayed that nicotine-selective affinity induced by the use of TFMAA was greater than that induce...

Cigarette smokers with brain damage involving the insular cortex display cessation of tobacco smoking, suggesting that this region may contribute to nicotine addiction. In the present study, we speculated that molecules in the insular cortex that are sensitive to experimental traumatic brain inj...

A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives was synthesized, and their structure–activity relationships were examined in order to identify potent and selective arginine vasopressin V2 receptor agonists. Attempts to substitute other chemical group...

[(Methyl-pyridin-2-ylmethyl-amino)-methyl]-phosphonic acid is a new bifunctional chelator for the fac-[99mTc(CO3)]+ core which can be linked to biomolecules via formation of phosphonic acid esters. Its synthesis and the coupling to model alcohols and to a bioactive molecule (cobinamide) are desc...

Two minor ether-soluble resin glycosides, scamrnonins VII and VIII, were isolated from Radix Scammoniae, the roots of Convolvulus scammonia. In addition to (2S)-2-methylbutyric acid and tiglic acid, they are composed, respectively, of orizabic acid A and a new glycosidic acid named scammonic aci...

Four kinds of ether-soluble resin glycosides named scammonins III–VI were obtained as their acetates from Radix Scammoniae (scammony root), the root of Convolvulus scammonia. Their structures have been determined on the bases of chemical and spectral evidences. All of them have a common glycosi...

The ether-soluble resin glycoside (‘jalapin’) fraction obtained from scammony roots, on alkaline hydrolysis, gave a glycosidic acid, scammonic acid A, together with isobutyric, 2S-methylbutyric and tiglic acids. In addition, two kinds of resin glycosides, named scammonin I and II, were isolate...

This study compared the effects of simendan, a calcium sensitizer, with those of milrinone and enalapril on survival of rats with healed myocardial infarction. Seven days after ligation-induced myocardial infarction, the rats were randomized to control, milrinone, enalapril, or simendan groups. ...

Objective.A phase II study was conducted to determine the efficacy of single agent flavopiridol therapy in patients with recurrent or persistent endometrial adenocarcinoma refractory to established treatments.

Flavopiridol (FP), a synthetic flavone, is a cyclin-dependent kinase inhibitor and possesses an anti-cancer activity. The effect of FP on interferon (IFN)-γ-induced nitric oxide (NO) production in mouse vascular endothelial cell line END-D was examined. FP significantly inhibited IFN-γ-induced...

Typical mantle cell lymphoma (MCL) is a distinct B-cell non-Hodgkin's lymphoma associated with over-expression of cyclin D1 related to translocation between the IgH and BCL-1 genes. Due to the important functional interaction between cyclin D1 and cyclin dependent kinases, cyclin dependent ...

Flavonoids have been discovered as novel inhibitors of glycogen phosphorylase (GP), a target to control hyperglycemia in type 2 diabetes. To elucidate the mechanism of inhibition, we have determined the crystal structure of the GPb-chrysin complex at 1.9 Å resolution. Chrysin is accommodated at ...