A convenient route for the synthesis of some 2-propen-1-one derivatives with E isomeric configuration is described. The activity of the synthesized compounds was evaluated through behavioral studies of apomorphine-induced licking in animal models. It was demonstrated that most of the synthesized...

The binding of isothipendyl hydrochloride (IPH) to bovine serum albumin (BSA) was investigated by fluorescence spectroscopy combined with UV–visible absorption and circular dichroism (CD) techniques under simulative physiological conditions for the first time. The quenching mechanism of fluores...

Reactivity of magnesium phthalocyanine (MgPc) in the dry 3,5-lutidine (3,5-lut), in the 3,5-lut/DMSO and in 3,5-lut/acetylacetone (acacH) systems has been investigated. Reaction of MgPc with dry 3,5-lut leads to formation of MgPc(3,5-lut)2 compound (1), in which the Mg atom is characterized by r...

Novel coordination compounds of Cu(II) with tris(3,5-dimethylpyrazol-1-yl)methane (HC(3,5-me2pz)3) such as [Cu(HC(3,5-me2pz)3)2][CuCl4]·2H2O (I) and [Cu(HC(3,5-me2pz)3)2][Cu2Br6]·4H2O (II), have been synthesized. These compounds were studied by IR and electronic (SDR) spectroscopy. It has been...

Two regioselective synthetic routes towards 3,5-disubstituted isoxazoles from ynones are reported. One route takes place via first converting the ynones to ynone O-methyl oximes, followed by a palladium-catalyzed intramolecular cyclization. The other involves the formation of 5-hydroxy-4,5-dihyd...

Systematic identification and quantification of active radical sites in a small molecule, pyrazolium 3,5-dinitrobenzoate:3,5-dinitrobenzoic acid as well as in the stable free radical (DPPH•) were carried out by Fukui functions calculation using DFT functional with B3LYP/6–311++G(d,p) level of b...

Although the tricyclic antidepressant drugs imipramine and doxepin exert similar direct electrophysiological effects on cardiac cells, toxic cardiac arrhythmias and conduction disturbances are much more commonly associated with imipramine than doxepin in clinical use. To ascertain if this discre...

□ Two chromatographic methods, high-performance liquid chromatography (HPLC) and high-performance thin-layer chromatography (HPTLC) were compared for sensitivity and reproducibility in the analysis of the tricyclic antidepressant doxepin and its metabolite, desmethyldoxepin, in plasma. The HPLC...

A GLC method for the simultaneous quantitative determination of the cis- and irarrs-isomers of doxepin and desmethyldoxepin in human plasma was developed. The method involves the use of a capillary column for efficient separation of the four compounds and the internal standards, amitriptyline an...

Doxepin is a tricyclic antidepressant marketed as an irrational mixture of cis- and trans-geometric isomers in the ratio of 15:85. A convenient high-performance liquid chromatographic (HPLC) procedure for simultaneous quantitation of geometric isomers of doxepin and N-desmethyldoxepin in plasma ...

The thermodynamic pKa values for doxepin and its metabolite desmethyldoxepin were determined by the solubility method to be 8.96 and 9.75, respectively at 25°. The intrinsic solubilities for doxepin and desmethyldoxepin were linearly dependent upon ionic strength. The intrinsic solubilities at ...

A sensitive method for the simultaneous determination of doxepin and its active metabolite desmethyldoxepin in plasma was established, using high-performance liquid chromatographic separation with tandem mass spectrometric detection. The samples were extracted with hexane–isoamyl alcohol, separ...

5α-Androstane-3, 16-dione has been prepared by hydroboration and oxidation of 3β-hydroxy-5α-androst-16-ene. Reduction with sodium borohydride gave the 3β, 16β-diol. The fungus Cephalosporium aphidicola has been shown to hydroxylate 5α-androstane-3, 16-dione predominantly at the C-6β posit...

Stromal-epithelial relationships may be involved in the androgen-dependent development and maintenance of benign hyperplasia in the human prostate. Concentrations of endogenous 17β-hydroxy-5α-androstan-3-one (DHT) have been determined in separated epithelial and stromal components of hyperplas...

Zusammenfassung5β-Androstan-3-one, die eine 6α-ständige Hydroxylgruppe besitzen, zeigen in ihren Massenspektren ein Schlüsselion, das dem Verlust von Wasser und der C-Atome 1–4 als C4H5O•-Teilchen entspricht. Bei den analogen 6β-Isomeren wird hingegen C-1 bis C-4 als C4H7O•-Teilchen abgespa...

The topical anti-androgen 17β-hydroxy-1α-methyl-17α-propyl-5α-androstan-3-one is determined in plasma samples by extracting with ether and subsequent mass fragmentography with single-ion detection at m/z 303. 17 β-Hydroxy-1α-methyl-17α-pentyl-5α-androstan-3-one, added to the samples befo...

Metabolism of 5α-androstan-3-one in the rabbit was studied in order to investigate changes in the steroidal ring system. The total crude urinary extract was separated into a non-ketonic and a ketonic fraction and was further purified by column chromatography. 3α- and 3β-Hydroxy-5α-androstan-...

The neutral urinary excretion products of 17β-hydroxy-2α-methyl-5α-androstan-3-one from the rabbit dosed orally were investigated. Together with oxidation-reduction of the oxygen functions at C-3 and C-17 hydroxylation occurred at C-15, C-16, and at the 2α-methyl positions of the steroid nuc...

Type 3 17β-hydroxysteroid dehydrogenase (17β-HSD), a key steroidogenic enzyme, transforms 4-androstene-3,17-dione (Δ4-dione) into testosterone. In order to produce potential inhibitors, we performed solid-phase synthesis of model libraries of 3β-peptido-3α-hydroxy-5α-androstan-17-ones with...

An acidic metabolite, 2α-carboxy-5α-androstane-3α, 16α, 17αtriol and two neutral metabolites, 2α-hydroxymethyl-5α-androstane-3α, 17α-diol, and 2α-hydroxymethyl-5α-androstane-3α, 16α, 17α-triol have been identified in the urine of rabbits orally dosed with 17β-hydroxy-2-hydroxymeth...