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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Sci. Pharm., Volume 69, Issue 4 (December 2001) – 13 articles , Pages 257-388

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Article
ALKALOIDS FROM OXYTROPIS MYRIOPHYLLA (PALL) DC
Sci. Pharm. 2001, 69(4), 383-388; https://doi.org/10.3797/scipharm.aut-01-208 - 28 Dec 2001
Cited by 8 | Viewed by 876
Abstract
Five alkaloids were isolated from the epigeal part of Oxytropis myriophylla. Three alkaloids were identified as N-benzoyl-β-phenylethylamine, N-trans-cinnamoyl-β-phenylethylamine, N-cis-cinnamoyl-β-phenylethylamine and the structures of two new alkaloids were elucidated to be N-benzoyl-β-hydroxyphenylethylarnine(2), N-trans-cinnamoyl-β-hydroxy-phenylethylamine
(5). The absolu.te structures were established by modified Mosher method. Full article
Article
Aufnahme ausgewählter Metalle in Kompartimente von Solanaceen
by , and
Sci. Pharm. 2001, 69(4), 375-382; https://doi.org/10.3797/scipharm.aut-01-207 - 28 Dec 2001
Cited by 1 | Viewed by 501
Abstract
The Uptake of several metals into the compartments of Atropa belladonna, Datura stramoni-um, and Hyoscyamus niger is measured by ICP-AES. In the roots the series AI < Ba < Cr < Cu< Zn < Sr is observed. Full article
Article
Utilization of hydralazine hydrochloride in the Potentiometric Determination of Osmium(VIII): Analysis of Binary and Ternary Mixtures
by and
Sci. Pharm. 2001, 69(4), 367-374; https://doi.org/10.3797/scipharm.aut-01-206 - 28 Dec 2001
Cited by 2 | Viewed by 510
Abstract
A simple, rapid and accurate potentiolnetric method is described for tlie
determination of Os(VIII) in tlie co~icentrationr ange 0.4-4.0 mg/ml. Tlie method is
based on tlie addition of hydralazine hydrochloride to Os(VIII) to reduce it to Os
(IV). The excess of hydralazine hydrocliloridew [...] Read more.
A simple, rapid and accurate potentiolnetric method is described for tlie
determination of Os(VIII) in tlie co~icentrationr ange 0.4-4.0 mg/ml. Tlie method is
based on tlie addition of hydralazine hydrochloride to Os(VIII) to reduce it to Os
(IV). The excess of hydralazine hydrocliloridew as oxidized by iodine dissolved ill acetic acid. The liberated iodide was then potentiometrically titrated against mercury(II) using silver amalgam as the indicator electrode. The potential of this method for sime- microdetermination is important in practical applications where tlie above reaction should proceed quantitatively towards completion. The relative standard deviation for six replicate deterinination of osmium(VIII) in binary and
ternary mixtures without the need for extraction or heating. Full article
Article
Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs
Sci. Pharm. 2001, 69(4), 351-366; https://doi.org/10.3797/scipharm.aut-01-205 - 28 Dec 2001
Cited by 14 | Viewed by 620
Abstract
A new series of 4(3H)-quinazolinone analogs bearing 6-iodo and 2-thioether functions were synthesized and screened for their in vitro antitumor activity. Eight compounds were identified as active anticancer agents. 2-Mercapto-3-benzyl-4-thioxo-6-iodo-3H-quinazolin (2) and 2-(2,4-dinitrophenyl)-3-benzyl-6-iodo-4-(3H)-quinazolinone(9) [...] Read more.
A new series of 4(3H)-quinazolinone analogs bearing 6-iodo and 2-thioether functions were synthesized and screened for their in vitro antitumor activity. Eight compounds were identified as active anticancer agents. 2-Mercapto-3-benzyl-4-thioxo-6-iodo-3H-quinazolin (2) and 2-(2,4-dinitrophenyl)-3-benzyl-6-iodo-4-(3H)-quinazolinone(9) proved to be the most active compounds in this study. They showed MG-MID GI50, TGI, LC50 values of 3.9, 25.2, 82.3 and 2.7, 12.3, 38.7 μM, respectively. The detailed synthesis and biological screening data are reported. Full article
Article
Synthesis, Selective Aldose Reductase Inhibitory Profile and Antihyperglycaemic Potential of Certain Parabanic Acid Derivatives
by , , and
Sci. Pharm. 2001, 69(4), 329-350; https://doi.org/10.3797/scipharm.aut-01-204 - 28 Dec 2001
Cited by 4 | Viewed by 945
Abstract
Synthesis and aldose reductase inhibitory profile of certain parabanic acid derivatives 1a-p is described. Also, the antihyperglycaemic potential of these compounds was studied. The most active inhibitors in this series were compounds 1g, 1p, and 10 which showed inhibitory [...] Read more.
Synthesis and aldose reductase inhibitory profile of certain parabanic acid derivatives 1a-p is described. Also, the antihyperglycaemic potential of these compounds was studied. The most active inhibitors in this series were compounds 1g, 1p, and 10 which showed inhibitory activity, 36.6,90 and 91% respectively, at concentration 1 x 1 0−4. Their IC50 were 2 x 10−6, 7.5 x 1 0-8 and 5 x 10-8, respectively. Compound 10 exhibited pronounced antihyperglycaemic effect. Full article
Article
Synthese von einigen potentiellen NO-Synthase-Inhibitoren mit Thieno[2,3-b] [1,4l thiazin-Grundgerüst
by , and
Sci. Pharm. 2001, 69(4), 321-328; https://doi.org/10.3797/scipharm.aut-01-203 - 28 Dec 2001
Cited by 2 | Viewed by 552
Abstract
The synthesis of thiolactime 4 and first studies on the syntheses of other thiolactimes with different substituted thieno[2,3-b][1,4]thiazine moieties are described as well as the syntheses of structurally modified amidines 10 - 14 with the same basic structure. The thieno[2,3-b][1,4]thiazine derivatives were prepared [...] Read more.
The synthesis of thiolactime 4 and first studies on the syntheses of other thiolactimes with different substituted thieno[2,3-b][1,4]thiazine moieties are described as well as the syntheses of structurally modified amidines 10 - 14 with the same basic structure. The thieno[2,3-b][1,4]thiazine derivatives were prepared by reacting methyl 5-chloro-4-nitro-2-thiophencarboxylate with ethyl thioglycolate followed by reductive cyclisation to 6, which was either first saponified and then treated with Lawesson reagent to obtain thiolactame 8 or directly reacted to thiolactame 9. Reaction of 9 with various amines led to the desired products 10 - 14. which will undergo pharmacological testing on NO synthase inhibiting activities. Full article
Article
DENSITOMETRTSCHE UNTERSUCHUNGEN ZUR PHOTOSTABILITÄT VON MELOXICAM
by , , and
Sci. Pharm. 2001, 69(4), 315-320; https://doi.org/10.3797/scipharm.aut-01-202 - 28 Dec 2001
Cited by 1 | Viewed by 556
Abstract
Photodegradation of meloxicam is studied placing special emphasis on the investigation of the correlation between the sample concentration and the stability. For quantitation a HPTLC assay was developed. The stability indicating capability ofthe assay is proved using a sampie solution exposed to artificial [...] Read more.
Photodegradation of meloxicam is studied placing special emphasis on the investigation of the correlation between the sample concentration and the stability. For quantitation a HPTLC assay was developed. The stability indicating capability ofthe assay is proved using a sampie solution exposed to artificial irradiation from a xenon source, the peak of meloxicam was weil separated from all
degradation products. For quantitation external calibration is employed. Sample solutions of meloxicam of three different concentrations (2 mg ml-1; 250 μg ml-1 ; 40 μg ml-1) are subjected to simulated sunlight and tested for stability. Full article
Article
KAPILLARELEKTROPHORETISCHE BESTIMMUNG VON KOHLENHYDRAT-ENANTI0MEREN
by and
Sci. Pharm. 2001, 69(4), 299-314; https://doi.org/10.3797/scipharm.aut-01-201 - 28 Dec 2001
Viewed by 694
Abstract
Capillary electrophoresis is a versatile analytical technique for the determination of a very widespread range of compounds. Many applications for the separation of different pharmaceuticals, ions, herbicides and biomolecules such as DNA, proteins and peptides have been published over the last decade. A [...] Read more.
Capillary electrophoresis is a versatile analytical technique for the determination of a very widespread range of compounds. Many applications for the separation of different pharmaceuticals, ions, herbicides and biomolecules such as DNA, proteins and peptides have been published over the last decade. A comparatively new field is the separation and determination of carbohydrates by
capillary electrophoresis, especially the assignment of absolute configuration. These methods will also gain importance in the field of pharmaceutical carbohydrate analysis. In this review a short overview ofthe different methods and separation procedures is given and some applications for the separation of sugar enantiomers are described in more detail. Full article
Article
Zytoprotektion mit Amifostin (Ethyol®) in der Chemotherapie: Meta-Analyse zum pharmakokinetischen Interaktionspotential mit Zytostatika
by , and
Sci. Pharm. 2001, 69(4), 289-297; https://doi.org/10.3797/scipharm.aut-01-200 - 28 Dec 2001
Viewed by 1153
Abstract
The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the influence of AMI on the pharmacokinetics of different cytostatics [...] Read more.
The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the influence of AMI on the pharmacokinetics of different cytostatics was investigated. Preadministration of AMI increased Cmax of doxorubicin (+ 44 %, p < 0.06), epirubicin (+ 31 %, P < 0.08), mitomycin C (+ 41 %, p < 0.01) and docetaxel (+ 31 % and + 17 %, not significant). In contrary, the peak concentration of pirarubicin , the tetrahydropyranyl-prodrug of doxorubicin was decreased (- 50 %, P < 0.03), leading to an equal higher concentration
of doxorubicin in the blood . In accordance to the peak concentrations, the AUC'ast was increased by chemoprotection: doxorubicin + 53 % (p < 0.01) and epirubicin + 23 % (not significant), docetaxel + 25 % and + 31 % (not significant). AUC'ast of mitomycin C and paclitaxel seemed to be unaffected by preadministered AMI. A particular inhibition of the protein binding by AMI has been identified as one reason for higher serum concentrations of anthracycline drugs. After cytoprotection, a possible increase of the cytostatic's Serum concentrations should be taken into account for optimal dosage schedules. Full article
Article
Zur Farbreaktion von Amiloridhydrochlorid Ph. Eur.
Sci. Pharm. 2001, 69(4), 275-287; https://doi.org/10.3797/scipharm.aut-01-199 - 28 Dec 2001
Cited by 1 | Viewed by 637
Abstract
The reaction of amiloride hydrochloride (1.HCI) with bromine in alkaline solution generated a yellow-brown dehydrogenation product, which tumed out as 3-(3-amino-I,2,4-oxadiazol-5-yl)-5-chloro-2,6-pyrazinediamine (2). The structure was deduced from the MS and the NMR spectra of 2 with the help of comparisons with [...] Read more.
The reaction of amiloride hydrochloride (1.HCI) with bromine in alkaline solution generated a yellow-brown dehydrogenation product, which tumed out as 3-(3-amino-I,2,4-oxadiazol-5-yl)-5-chloro-2,6-pyrazinediamine (2). The structure was deduced from the MS and the NMR spectra of 2 with the help of comparisons with corresponding spectra of amiloride (1) and reference substances 3 - 5. The agreement of all relevant data of the product and of authentical oxadiazolylpyrazine 2 as weil as the accomplished X-ray analysis confirmed the postulated structure. The mechanism of the formation of 2 is also discussed. Full article
Article
Sulfonylanaloge Spirohydantoine
by and
Sci. Pharm. 2001, 69(4), 271-274; https://doi.org/10.3797/scipharm.aut-01-198 - 28 Dec 2001
Cited by 1 | Viewed by 588
Abstract
New thiasubstituted sulfonyl analogues of spirohydantoins were synthesized and tested for their anticonvulsant effects. In low concentrations they had no anticonvulsant activities, in higher ones they were neurotoxic. Full article
Article
Synthese, Reaktivität und fungizide Eigenschaften von 4-Hydroxy(Alkoxy)iminooxazolidin-2-onen
by and
Sci. Pharm. 2001, 69(4), 265-270; https://doi.org/10.3797/scipharm.aut-01-197 - 28 Dec 2001
Cited by 4 | Viewed by 596
Abstract
4-Hydroxyimino-oxazolidin-2-ones (3) were prepared by hydroxylaminolysis of 4-alkoxy-3-oxazolin-2-ones (2). Treatment of 3a with ethyl chloroformate in a molar ratio of 1:1 afforded 6, whereas the reaction 3a with two equivalents of ethyl chloroformate produced 4 and 5 [...] Read more.
4-Hydroxyimino-oxazolidin-2-ones (3) were prepared by hydroxylaminolysis of 4-alkoxy-3-oxazolin-2-ones (2). Treatment of 3a with ethyl chloroformate in a molar ratio of 1:1 afforded 6, whereas the reaction 3a with two equivalents of ethyl chloroformate produced 4 and 5. By reacting 3a,d with diphosgene or thiophosgene the novel tetrahydro-oxazolo[ 4,3-c]1 ,2,4-oxadiazoles 7 could be
obtained in low yields. From the prepared novel compounds only 3a displayed a remarkable fungicidal activity at 2 ppm. Full article
Article
Tetramethyltetrahydro-1,4-anthrachinonazobenzoesäure, ein 5-Lipoxygenase-Inhibitor mit zelldifferenzierender Aktivität.
Untersuchungen an 1,4-Naphthochinonen, 28. Mitt. 1)
by , and
Sci. Pharm. 2001, 69(4), 257-264; https://doi.org/10.3797/scipharm.aut-01-196 - 28 Dec 2001
Viewed by 600
Abstract
The combination of 5-lipoxygenase (5-LOX) inhibition and retinoid activity in one molecule could be a suitable too1 for the topical psoriasis therapy. The anellation of the 5-LOX inhibitor 1 with the tetramethylcyclohexane moity to the arotinoid structure 2 does not fullfil this expectation. [...] Read more.
The combination of 5-lipoxygenase (5-LOX) inhibition and retinoid activity in one molecule could be a suitable too1 for the topical psoriasis therapy. The anellation of the 5-LOX inhibitor 1 with the tetramethylcyclohexane moity to the arotinoid structure 2 does not fullfil this expectation. This compound was not able to differentiate HL-60 cells to granulocytes. The exchange of the 3,5-di-tertbutyl-
4-hydroxyphenyl substituent by benzoic acid and the synthesis of 8 resulted in the loss of 5-LOX inhibition also. The construction of 10 by the introduction of an azo spacer between the anthraquinone moity and benzoic acid of 8 finally led to the expected compound: 10 was potent 5-LOX inhibitor and concomitant differentiated HL-60 cells as measured by the NBT test. Full article
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