Next Issue
Volume 70, March
Previous Issue
Volume 69, September
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
6.4
2.5
Journals
Sci. Pharm.
Volume 69
Issue 4
share announcement
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

  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list.
  • You may sign up for e-mail alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Reader to open them.
Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
1688 KiB  
Article
ALKALOIDS FROM OXYTROPIS MYRIOPHYLLA (PALL) DC
by Keisuke Kojima, Purevsuren S., Narantuya S., Tsetsegmaa S., Jamyansan Ya, Kimio Lsaka and Yukio Ogihara
Sci. Pharm. 2001, 69(4), 383-388; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-208 - 28 Dec 2001
Cited by 9 | Viewed by 1285
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
2963 KiB  
Article
Aufnahme ausgewählter Metalle in Kompartimente von Solanaceen
by D. Riße, H. Lahl and B. Unterhalt
Sci. Pharm. 2001, 69(4), 375-382; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-207 - 28 Dec 2001
Cited by 1 | Viewed by 697
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
2967 KiB  
Article
Utilization of hydralazine hydrochloride in the Potentiometric Determination of Osmium(VIII): Analysis of Binary and Ternary Mixtures
by A. S. Amin and H. M. Saleh
Sci. Pharm. 2001, 69(4), 367-374; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-206 - 28 Dec 2001
Cited by 2 | Viewed by 717
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
3977 KiB  
Article
Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs
by S. G. Abdel Hamid, H. A. El-Obeid, K. A. Al-Rashood, A. A. Khalil and H. I. El-Subbagh
Sci. Pharm. 2001, 69(4), 351-366; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-205 - 28 Dec 2001
Cited by 14 | Viewed by 954
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
6679 KiB  
Article
Synthesis, Selective Aldose Reductase Inhibitory Profile and Antihyperglycaemic Potential of Certain Parabanic Acid Derivatives
by M. Nabil Aboul-Enein, A. EI-Azzouny, Y. A. Maklad and M. I. Attia
Sci. Pharm. 2001, 69(4), 329-350; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-204 - 28 Dec 2001
Cited by 5 | Viewed by 1435
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
2211 KiB  
Article
Synthese von einigen potentiellen NO-Synthase-Inhibitoren mit Thieno[2,3-b] [1,4l thiazin-Grundgerüst
by M. E. Galanski, N. Böhler and T. Erker
Sci. Pharm. 2001, 69(4), 321-328; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-203 - 28 Dec 2001
Cited by 1 | Viewed by 780
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
1883 KiB  
Article
DENSITOMETRTSCHE UNTERSUCHUNGEN ZUR PHOTOSTABILITÄT VON MELOXICAM
by H. Bartsch, A. Eiper, B. Göls and H. Kopelent-Frank
Sci. Pharm. 2001, 69(4), 315-320; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-202 - 28 Dec 2001
Cited by 1 | Viewed by 828
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
4869 KiB  
Article
KAPILLARELEKTROPHORETISCHE BESTIMMUNG VON KOHLENHYDRAT-ENANTI0MEREN
by B. Lachmann and C. R. Noe
Sci. Pharm. 2001, 69(4), 299-314; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-201 - 28 Dec 2001
Viewed by 945
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
2397 KiB  
Article
Zytoprotektion mit Amifostin (Ethyol®) in der Chemotherapie: Meta-Analyse zum pharmakokinetischen Interaktionspotential mit Zytostatika
by Martin Czejka, Johannes Schüller and Heidemarie Kletzl
Sci. Pharm. 2001, 69(4), 289-297; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-200 - 28 Dec 2001
Viewed by 1498
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
4249 KiB  
Article
Zur Farbreaktion von Amiloridhydrochlorid Ph. Eur.
by Klaus Görlitzerl, Silke Huth, Peter G. Jones, Edith Gößnitzer and Winfried Wendelin
Sci. Pharm. 2001, 69(4), 275-287; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-199 - 28 Dec 2001
Cited by 1 | Viewed by 932
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
1281 KiB  
Article
Sulfonylanaloge Spirohydantoine
by B. Unterhalt and A. Scheppan
Sci. Pharm. 2001, 69(4), 271-274; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-198 - 28 Dec 2001
Cited by 1 | Viewed by 809
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
2282 KiB  
Article
Synthese, Reaktivität und fungizide Eigenschaften von 4-Hydroxy(Alkoxy)iminooxazolidin-2-onen
by Detlef Geffken and Cordula Riederer
Sci. Pharm. 2001, 69(4), 265-270; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-197 - 28 Dec 2001
Cited by 5 | Viewed by 838
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
2176 KiB  
Article
Tetramethyltetrahydro-1,4-anthrachinonazobenzoesäure, ein 5-Lipoxygenase-Inhibitor mit zelldifferenzierender Aktivität.
Untersuchungen an 1,4-Naphthochinonen, 28. Mitt. 1)
by G. Wurm, R. Probst and S. Schwandt
Sci. Pharm. 2001, 69(4), 257-264; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-01-196 - 28 Dec 2001
Viewed by 840
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
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-13
Previous Issue
Next Issue
Back to TopTop