The molecular structures of 1-(4-dimethylaminopyridinium)-2-bromo-1,1,2,2-tetrafluoroethane bromide (1-Br) (triclinic, P1̄, a=538.80(10), b=916.6(3), c=1372.8(3) pm, α=81.56(2)°, β=81.76(2)°, γ=82.53(2)°) and 1-(4-dimethylaminopyridinium)-1,1,2,2-tetrafluoroethane bromide (2-Br) (monoclini...

A small library of novel copper and zinc imidazo[1,2-a]pyridine complexes have been synthesized. Their structures were confirmed by X-ray diffraction crystallography and a selection of these compounds was tested against five cancer cell lines originating from breast cancer (MCF-7 and MDA-MB-231)...

Objective To determine the short-term safety and tolerability of the addition of ecadotril to conventional therapy in patients with mild to moderate heart failure. Methods Fifty ambulatory patients, 18 to 75 years of age, with mild to moderate heart failure, left ventricular ejection fraction ≤...

The hyperpolarization-activated transient current of mammalian 5-hydroxytryptamine transporters (SERT) expressed in Xenopus oocytes was studied. Human (h) and rat (r) SERT transient currents are blocked by HEPES with changes in the waveform kinetics, and the blockade of hSERT has use-dependent p...

Short and stereoselective syntheses of the two hydroxylated polyunsaturated fatty acid metabolites, namely 5-(S)-HETE and 5-(S)-HEPE, are reported in 23% and 30% overall yields, respectively. In addition, synthesis of the polyunsaturated fatty acid natural product (+)-zooxanthellactone has been ...

A series of myo-inositol 1,4,5-trisphosphate analogues with the 2-acyl substituents p-aminobenzoyl (7), p-azidobenzoyl (8), 4-{5-[2-(benzamido)ethyl]-2-hydroxyphenylazo}benzoyl (9), and cis,trans-4-aminocyclohexylcarbonyl (10) were synthesised and examined for their effects on the 5-phosphatase,...

Injection of inositol 1,4,5-trisphosphate (Ins 1,4,5-P3) into Limulus ventral photoreceptors produces excitation similar to that produced by light. One process which might contribute to rapid termination of the responses to Ins 1,4,5-P3 and to light is the hydrolysis of Ins 1,4,5-P3 by an InsP3-...

Lipid microparticles (LMs) as a sustained release system for a gonadotropin release hormone (GnRH) antagonist (Antide) were prepared and evaluated. Antide loaded microparticles (Antide–LMs) were obtained by a cryogenic micronization process starting from two different monoglycerides (glyceryl m...

This study evaluated the fasted state gastrointestinal behavior of the lipophilic drug itraconazole, orally administered to healthy volunteers as either a solid dispersion (Sporanox® capsules) or a cyclodextrin-based solution (Sporanox® solution). Following intake of the drug products, gastric a...

Itraconazole (ITZ) is a first-generation triazole-containing antifungal agent that effectively treats various fungal infections. As ITZ has a better safety profile than that of ketoconazole (KCZ), ITZ has been used worldwide for over 25 years. However, few reports have explored the metabolic pro...

SummaryThe concentrations of itraconazole and its active metabolite, hydroxy-itraconazole, were determined in the sera of 49 patients having received itraconazole for therapeutic or prophylactic purposes. Measurements by HPLC were compared with a biological assay using a strain of Paecilomyces v...

In a previously performed small-scale clinical study, healthy volunteers were asked to ingest an oral solution of itraconazole (Sporanox®) containing 40% 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) (i) with or (ii) without a standardized volume of water (240 mL) after which gastrointestinal and b...

A reversed phase ultra-performance liquid chromatography method was developed for the simultaneous quantitative determination of the systemically administered azoles voriconazole, posaconazole, isavuconazole, itraconazole and its metabolite hydroxy-itraconazole in plasma. The method involved a s...

BackgroundThe pharmacokinetic variability of hydroxy-itraconazole (OH-ITZ), an active metabolite of itraconazole (ITZ), is not fully known.

A chromatographic method (high-performance liquid chromatography/photodiode array detection) for the simultaneous determination of itraconazole and its mayor metabolite, hydroxy itraconazole, was developed. The validation data demonstrated acceptable values for linearity (dynamic range between 0...

A highly sensitive, selective, and precise ultra-performance liquid chromatography tandem mass spectrometry method was developed and validated for simultaneous quantification of itraconazole and hydroxy itraconazole in human plasma by a single liquid–liquid extraction step. The precursor to pro...

A high-performance liquid chromatography tandem mass spectrometry (LC–MS/MS) assay was developed and validated for simultaneous determination of itraconazole (ITZ), hydroxy-itraconazole (OH-ITZ), keto-itraconazole (keto-ITZ) and N-desalkyl itraconazole (ND-ITZ) concentration in human plasma. On...

IntroductionInvasive fungal infections are an increasing cause of mortality and morbidity in high risk patient populations such as those on immunosuppressive therapy. Triazole antifungals are recommended for the prevention and treatment of such infections.The aim of this study was to develop and...

A convenient method was reported to synthesize 3-(4′-nitrophenyl)iminocoumarin by a cyclization reaction following a Knoevenagel reaction of 2-hydroxybenzaldehyde with 4-nitrophenylacenitrile in an ethanol solution. Piperidine or piperazine was employed respectively as catalyst. Crystal structu...

Anti-(4-hydroxy-3-nitrophenyl)acetyl (NP) antibodies bearing λ1 chains are known to possess fine specificity, referred to as heterocliticity, which causes these antibodies to bind to hapten analogues such as (4-hydroxy-3-iodo-5-nitrophenyl)acetyl (NIP) and (4-hydroxy-3,5-dinitrophenyl)acetyl (N...