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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 1 (March 2001) – 11 articles , Pages 1-104

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Article
Parameters influencing the transport rate of marker compounds across Caco-2 monolayers
by , and
Sci. Pharm. 2001, 69(1), 91-104; https://doi.org/10.3797/scipharm.aut-01-11 - 30 Mar 2001
Cited by 1 | Viewed by 628
Abstract
Performing transport experiments with Caco-2 monolayers some important parameters have to be considered. Cell layers are appropriate for transport studies after complete polarisation and differentiation. Consequently they should be used 20 - 25d after seeding. Monolayers grown for shorter time than 20d yield
[...] Read more.
Performing transport experiments with Caco-2 monolayers some important parameters have to be considered. Cell layers are appropriate for transport studies after complete polarisation and differentiation. Consequently they should be used 20 - 25d after seeding. Monolayers grown for shorter time than 20d yield to high transport rates, a cultivation period longer than 25d results in layers susceptible to detachment. Additionally the material of the filter support exerts an influence on the transport data because of varying barrier functions of cell layers grown on polyester- versus polycarbonate filter inserts. By comparison of transport rates obtained with different model systems such as Transwells and Ussing chambers the influence of the unstirred water layer on permeation of markers was investigated. The results indicate that there is a noticeable difference with hydrophobic compounds only. To check the dependence of transport phenomena on energy the difference in transport rates between 4°C and 37°C as well as the cumulative transport subject to the transport direction was determined. Moreover the influence of the stirring rate on the cumulative transport in the Ussing chamber system was elucidated. For assessment of the cell associated amount of the transported substance the cell layer was dissolved in NaOH / SDS to get further valuable informations.
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Article
Analysis, Chemotype and Quality Control of the Essential Oil of a New Cultivated Basil (Ocimum basilicum L.) Plant from Bulgaria
Sci. Pharm. 2001, 69(1), 85-89; https://doi.org/10.3797/scipharm.aut-01-10 - 30 Mar 2001
Cited by 20 | Viewed by 1114
Abstract
The essential oil of the spice plant Ocimum basilicum L. (Lamiaceae) from Bulgaria was investigated using gas chromatographic-spectroscopic (GC/FID and GC/MS: polar, non-polar and chiral phases of GC columns) and olfactoric methods. As main compounds of this basil oil sample (R)-(-)-linalool (71.4%), (Z,E)-α-farnesene
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The essential oil of the spice plant Ocimum basilicum L. (Lamiaceae) from Bulgaria was investigated using gas chromatographic-spectroscopic (GC/FID and GC/MS: polar, non-polar and chiral phases of GC columns) and olfactoric methods. As main compounds of this basil oil sample (R)-(-)-linalool (71.4%), (Z,E)-α-farnesene (6.5%), 1,8-cineole (5.6%), τ-cadinol (2.8%), germacrene D (1.7%), citronellol (1.2%) and bornyl acetate (1.1%) were identified. Ths results show, that the essential basil oil from Bulgaria belongs to the European linalool chemotype. The correlations of olfactoric data (qualitative and quantitative) with the presented analytical ones certificate the good quality of this Bulgarian Ocimum basilicum sample. A possible use of this essential basil oil in medicine, perfumery and foods is discussed.
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Article
Flavonoids in Achillea collina
Sci. Pharm. 2001, 69(1), 75-83; https://doi.org/10.3797/scipharm.aut-01-09 - 30 Mar 2001
Cited by 8 | Viewed by 608
Abstract
In a detailed study on the flavonoid pattern of Achillea collina BECKER ten flavonoids were isolated from a methanolic extract of aerial parts of the plant. Their structures were determined by UV, ESI-MS, GC-MS and NMR spectroscopic methods including 2D-NMR. Apigenin-7-O-rutinoside was proven
[...] Read more.
In a detailed study on the flavonoid pattern of Achillea collina BECKER ten flavonoids were isolated from a methanolic extract of aerial parts of the plant. Their structures were determined by UV, ESI-MS, GC-MS and NMR spectroscopic methods including 2D-NMR. Apigenin-7-O-rutinoside was proven for the first time in the genus Achillea.
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Article
Triterpenoid saponins of Bellis perennis
by , , and
Sci. Pharm. 2001, 69(1), 69-73; https://doi.org/10.3797/scipharm.aut-01-08 - 30 Mar 2001
Cited by 10 | Viewed by 774
Abstract
Ten saponins have been isolated from the deacylated saponin mixture of Bellis perennis L. The structures of these saponins can be divided into two groups that show differences both in the aglycone and the carbohydrate moieties bound at C-28. The first group consists
[...] Read more.
Ten saponins have been isolated from the deacylated saponin mixture of Bellis perennis L. The structures of these saponins can be divided into two groups that show differences both in the aglycone and the carbohydrate moieties bound at C-28. The first group consists of glycosides of polygalacic acid with tri- or tetrasaccharide moieties consisting mainly of deoxyhexoses and a second group of glycosides of bayogenin or asterogenic acid which possess glucose as major carbohydrate moiety and one xylose or rharnnose unit. From the most polar fraction of the alkaline hydrolysate obtained from the underground parts of Bellis perennis one saponin possessing only glucose residues has been obtained. On the basis of a sugar methylation analysis and NMR spectral data, the structure was established as 3-O-ß-D-glucopyranosyl-2ß,3ß,23-trihydroxyolean-12-en-28-oic acid 28-O-ß-D-glucoyranosyl-(1→2)-[ß-D-glucopyranosyl(1→6)]-ß-D-glucopyranoside.
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Article
Diterpenoid Alkaloids from Consolida regalis S. F.Gray subsp.paniculata (Host) Soo var. paniculata
Sci. Pharm. 2001, 69(1), 63-67; https://doi.org/10.3797/scipharm.aut-01-07 - 30 Mar 2001
Cited by 5 | Viewed by 851
Abstract
Seven diterpenoid alkaloids : delcosine(1), delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var. paniculata. The presence of compounds 1,2,5,6 and 7 in this plant has not been previously reported.
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Article
6-, 7- AND 8-(5-ARY L-1-PHENYL-2-PYRAZOLIN-3-LY)IMIDAZO- AND PYRIMIDO[2,1-b]BENZOTHIAZOLES AS NOVEL ANTICONVULSANT AGENTS
by
Sci. Pharm. 2001, 69(1), 53-61; https://doi.org/10.3797/scipharm.aut-01-06 - 30 Mar 2001
Cited by 16 | Viewed by 680
Abstract
Some new derivatives of 2-amino-5- and 6-(5-aryl-1-phenyl-2-pyrazolin-3-yl)benzothiazole were synthesized from the corresponding aminophenyl compounds by reaction with KSCN/Br2 to build up the benzothiazole ring. The aminophenyl derivatives of pyrazoline were prepared by cyclization with phenylhydrazine of the appropriate 1,3-diphenyl-2-propen-1-one derivatives obtained from
[...] Read more.
Some new derivatives of 2-amino-5- and 6-(5-aryl-1-phenyl-2-pyrazolin-3-yl)benzothiazole were synthesized from the corresponding aminophenyl compounds by reaction with KSCN/Br2 to build up the benzothiazole ring. The aminophenyl derivatives of pyrazoline were prepared by cyclization with phenylhydrazine of the appropriate 1,3-diphenyl-2-propen-1-one derivatives obtained from arninoacetophenone and differently substituted aldehydes. However, the newly synthesized 2-aminobenzothiazole derivatives of pyrazoline were subjected to cyclization with ethyl brornopyruvate to afford the formation of 6- and 7-(5-aryl-1 -phenyl-2-pyrazolin-3 -yl)-2-ethoxycarbonylimidazo[2,1-b]benzothiazole derivatives. Furthermore, dimethyl acetylenedicarboxylate (DMAD) was used as another cyclizing agent for 2-aminobenzothiazole derivatives to obtain 7- and 8-(5-aryl-1-phenyl-2-pyrazolin-3-y1)-4-methoxycarbonyl-2-oxo-2H-pyrimido[2,1-b]benzothiazole derivatives. The newly prepared compounds were screened for their anticonwlsant activities. However, some of the tested compounds manifested good anticonvulsant potencies.
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Article
SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW 4H-PYRANO [3,2-h]QUINOLINES AND FUSED DERIVATIVES
Sci. Pharm. 2001, 69(1), 33-52; https://doi.org/10.3797/scipharm.aut-01-05 - 30 Mar 2001
Cited by 34 | Viewed by 826
Abstract
The starting materials, 2-amino-3-cyano-4-(3,4,5-trimethoxyphenyl)-4H-pyran0[3,2-hlquinoline 1 and ethyl-2-amino-4-(3,4,5-trimethoxyphenyl)-4H-pyrano [3,2-hlquinolin-3-carboxylate 2 were synthesised from 8-hydroxyquinoline and a-cyano-3,4,5-trimethoxycinnamonitrileand/or ethyl-a-cyano-3,4,5-trimethoxy-cinnamatre respectively. In order to construct a third heterocyclic ring 1 and 2were condensed with ethyl bromoacetate, formarnide, carbon disulfide to afford pyrrolo-, pyrimido- and thiazinopyranoquinolines 3 [...] Read more.
The starting materials, 2-amino-3-cyano-4-(3,4,5-trimethoxyphenyl)-4H-pyran0[3,2-hlquinoline 1 and ethyl-2-amino-4-(3,4,5-trimethoxyphenyl)-4H-pyrano [3,2-hlquinolin-3-carboxylate 2 were synthesised from 8-hydroxyquinoline and a-cyano-3,4,5-trimethoxycinnamonitrileand/or ethyl-a-cyano-3,4,5-trimethoxy-cinnamatre respectively. In order to construct a third heterocyclic ring 1 and 2were condensed with ethyl bromoacetate, formarnide, carbon disulfide to afford pyrrolo-, pyrimido- and thiazinopyranoquinolines 3-6respectively. The S-alkylated products 7 and 8 were obtained by the effect of chloroacetonitrile and/or ethyl chloroacetate on thiazinopyranoquinoline derivative 6. The attempt of cyanomethylation of the amino functional group of 1 to yield 10 with chloroacetonitrile in AcOHIAcONa failed and instead, pyridopyranoquinoline derivative 9 was obtained which is visualized to occur via cyclization of the initially formed acetylarnino derivative by nucleophilic attack on the cyano group. Acetylation of 1 and 2 with acetic anhydride afforded the mono- and di-acetyl derivatives 11a and 11b respectively. A plausible explanation to form the mono-derivative with 1 and the di-derivative with 2 is the higher deactivating effect of the cyano function over that of the carboxyethyl group. Furoylation of 1 and 2 was achieved by furoyl chloride to give 12a and 12b respectively. The structural features of pyranoquinoline 2 were inferred from its microanalysis and spectral data such as IR,1H-NMR and MS as well as its chemical reactions, as a bifunctional compound with carbon nucleophiles namely, phenyl isothiocyanate and nitrogen nucleophilic species namely, p-toluidine, benzylamine, aniline and hydrazine hydrate to give pyrimidopyranoquinoline derivative 13, carboxamides 14a-c and carboxyhydrazide 15 respectively. When the hydrazide 15 was treated with carbon disulfide inpresence of KOH, it afforded the potassium salt 16 which was submitted to react with hydrazine hydrate at room temperature to give 17. The hydrazido group of 15was utilized to construct heterocyclic moieties attached to postion-3 of the pyranoquinoline structure. Thus, the reaction of the carboxyhydrazide15 with phenyl isothiocyanate, acetylacetone, and benzoylacetone resulted in the formation of 18, 19a and 19b respectively. Ethyl carbazate as a typical mesophile reacted with 2 to afford a fused tetracyclic product triazepinopyranoquinoline 20 via cyclization of the initially formed hydrazide. Among sixteen compounds screened against E. coli and S. aureus respectively,compounds 2 and 14c show a high order of antibacterial activity against both bacteria. 12b is strongly potent against Staphylococcus aureus. Full article
Article
ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF 2-PHENYL (6, 8-DISUBSTITUTED 3,4-DIHYDRO-4-OXOQUINAZLIN-3-YCL) ACETO ACETAMIDES AND THEIR ß (4-SUBSTITUTED PHENYL) AZO ANALOGS
Sci. Pharm. 2001, 69(1), 27-32; https://doi.org/10.3797/scipharm.aut-01-04 - 30 Mar 2001
Cited by 1 | Viewed by 542
Abstract
2-phenyl-(3,4-dihydro-4-oxoquinazolin-3-yalc)e to acetamides (1&2) and their B-(4-substituted phenyl) azo derivatives (3-10) were evaluated for their analgesic and antiinflammatory activities. The bromophenyl azo derivative (4) showed significant activity as comparable to standard drugs viz pentazocine, aspirin and other compounds exhibited moderate activities. All the
[...] Read more.
2-phenyl-(3,4-dihydro-4-oxoquinazolin-3-yalc)e to acetamides (1&2) and their B-(4-substituted phenyl) azo derivatives (3-10) were evaluated for their analgesic and antiinflammatory activities. The bromophenyl azo derivative (4) showed significant activity as comparable to standard drugs viz pentazocine, aspirin and other compounds exhibited moderate activities. All the synthesized compounds were tested for their toxicity have not shown any abnormality up to 1500 mg/kg Body weight in experimental animals.
Full article
Article
Antiplatelet-Eigenschaften von 4-Oxo-4H-pyrazol-1,2-dioxiden
by and
Sci. Pharm. 2001, 69(1), 21-26; https://doi.org/10.3797/scipharm.aut-01-03 - 30 Mar 2001
Cited by 1 | Viewed by 530
Abstract
New 4-oxo-4H-pyrazol-1,2-dioxides were tested for their antiplatelet effects. Compound 2i has the highest activity in the Born test with 200 nMol/L. Full article
Article
Synthesis of Dioxigenated Systems. Preparation of Homologues of 1,4-Benzodioxin as Calcium Antagonists
Sci. Pharm. 2001, 69(1), 11-19; https://doi.org/10.3797/scipharm.aut-01-02 - 30 Mar 2001
Cited by 3 | Viewed by 666
Abstract
A new compound (9), homologue of 1,4-benzodioxin, has been prepared and tested as calcium antagonist. Additionally, the intermediates 12 and 13 with structure of aminodiol, were also evaluated as anticalcium agents. All of them showed a moderate anticalcium activity. Full article
Article
Darstellung und Atropisomerie von 1-[2-(2,2-Dimethylpiperidino)phenyl]ethanol
by and
Sci. Pharm. 2001, 69(1), 1-10; https://doi.org/10.3797/scipharm.aut-01-01 - 30 Mar 2001
Cited by 1 | Viewed by 561
Abstract
The title compound was prepared by Hg(II)-edta dehydrogenation of the aminoalkohol 2 via the benzoxazine 4, which reacted with methylmagnesiumiodide to 6. This compound shows in the NMR spectrum atropisomerism for the restricted rotation of the piperidine moiety about the aryl-C-N [...] Read more.
The title compound was prepared by Hg(II)-edta dehydrogenation of the aminoalkohol 2 via the benzoxazine 4, which reacted with methylmagnesiumiodide to 6. This compound shows in the NMR spectrum atropisomerism for the restricted rotation of the piperidine moiety about the aryl-C-N bond. The dehydrogenation of 6 stopped after a two electron withdrawal generating the benzoxazine 7, because the angular hydrogen atom occupies an equatorial position, which prevents stereoelectronic conditions for a further oxidation. Full article
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