bluuebunny/crossref_metadata_2025 huggingface dataset:
SISTEMA DE PRÁCTICAS PREPROFESIONALES E INTEGRACIÓN DE LAS FUNCIONES SUSTANTIVAS EN LAS CARRERAS DE EDUCACIÓN
Authors: Terranova Ruiz Jackeline Rosalía , Villafuerte Holguín Jhonny Saulo , Shettini Velásquez Teresa Elizabeth
Published: May 2019

El artículo que se presenta está dirigido a mejorar el sistema de la práctica profesional de las carreras de la Facultad Ciencias de la Educación de la Universidad Laica Eloy Alfaro de Manabí (Uleam). La misma, ha presentado serias deficiencias a consecuencias de la ausencia de una concepción holística de la práctica pre-profesional, como componente del proceso formativo de los estudiantes, futuros profesionales. En este sentido, se plantea determinar los componentes que sustentan el sistema de la práctica pre-profesional desde las funciones sustantivas como vía fundamental para elevar la calidad del graduado y la eficiencia académica de la Facultad de Ciencias de la Educación de la Uleam. Para ello, los métodos que se utilizaron en esta investigación son de carácter cuantitativo y cualitativo. De ahí que, con la investigación se logró implementar un sistema de práctica profesional integradora a través de una propuesta que fundamenta el desarrollo de la misma.
CIENCIA, TECNOLOGÍA Y SOCIEDAD: APORTES EN LA FORMACIÓN PROFESIONAL
Authors: Barcia Villamar Fabián Eduardo , Pico Pillasagua Juan Carlos , Macias Cedeño Paulo Emili
Published: May 2019

El ritmo creciente de la ciencia, tecnología, cultura y naturaleza crean nuevas formas de interpretación. En este artículo se argumenta una experiencia que permite comprender la ciencia y la tecnología contemporáneas como realizaciones culturales que rompen con las disociaciones tradicionales de estas, y redefinen, de algún modo, las mismas ideas de cultura y naturaleza, asimismo es capaz de fructificar en nuevas tecnologías culturales de interpretación, valoración e intervención. La formación del profesional actual requiere de adelantos del desarrollo científico que permitan garantizar el enfoque de ciencia, tecnología y sociedad como argumentos favorables que deben atenderse para poner en práctica como se expresa la necesidad de mejorar la calidad de vida del hombre.
DERMATOLOJİK HASTALIKLARDA ARAŞTIRMA YÖNTEMLERİ
Authors: Metintaş Selma , Atay Emrah
Published: May 2019

Bilimsel
yöntem, belli bir ‘sorunun’ belirlendiği, buna ilişkin bir ‘varsayımın’
biçimlendirildiği-formüle edildiği, bu çerçevede gözlem veya deneylerle
verilerin toplandığı ve varsayımın geçerliliğinin yargılandığı bir araştırma
dizgesidir. Bilimsel araştırmanın en özgün aşaması, varsayımın test edildiği
‘gerçekleştirme’ aşamasıdır. Araştırma tasarımları, geçerliliği ve
güvenilirliği en üst düzeye çıkaran ve yanlılık (bias) ya da hatayı en düşük
düzeye indiren araştırmaların sanatsal ve bilimsel yönüdür. Araştırma planlanmasında
dört temel kurgu ortaya çıkar: I- Gözlemsel araştırmalar II- Deneysel
araştırmalar, III- Metodolojik araştırmalar, IV-Sistematik derleme ve meta
analiz. Bu yazıda, dermatoloji hekimleri ve uzmanlık öğrencilerinin tıbbi
araştırma yöntemlerini tanımaları konusunda ön bilgi verilmesi amaçlandı.
BULAŞICI DERMATOLOJİK HASTALIKLARIN KONTROLÜ VE HALK SAĞLIĞI AÇISINDAN ÖNEMİ
Authors: Koku Aksu Ayşe Esra
Published: May 2019

Bulaşıcı
cilt hastalıkları birinci basamak sağlık kuruluşuna sık başvuru
sebeplerindendir. Bakteriyel, fungal ve paraziter hastalıklar gelişmekte olan
ülkelerde daha sık görülürken, viral hastalıklar ise gelişmiş ülkelerde ön
plana çıkmaktadır. Bakteriyel hastalıklardan en sık görülen piyodermidir,  mantar enfeksiyonlarından ise en sık görülen
dermatofitlerin etken olduğu yüzeyel mantar enfeksiyonlarıdır. Viral
hastalıklardan Herpes simpleks virüs, Varisella, Molluskum kontagiozum, verru,
paraziter hastalıklardan ise skabies ve pediküloz sık görülenler diğer bulaşıcı
cilt hastalıklarıdır. Hastalıkların dermatolojik bulgularının tanınması ile
erken tanı konulması sağlanabilir. Bulaş yolunun bilinmesi ile de hastalıkların
yayılması önlenebilir. Uygun izolasyon yöntemlerinin uygulanması bulaşın
azaltılmasında önem taşır.
Man, God, and Rain: Is Aristotelian Teleology Hierarchical?
Authors: Henrigillis Brandon
Published: May 2019

There are some passages within the Aristotelian corpus that indicate that Aristotle argued for a wider and more cosmic teleology than he is usually understood to have held.  There are two interpretive camps that have been formed as a response to these passages.  The first argues that Aristotle held only the internal teleology that he is commonly associated with, and the second argues that Aristotle must have defended a hierarchical teleology in which some things in the universe are meant to benefit other things.  I argue that both sides are mistaken, and that the key to understanding Aristotelian teleology is through a correct interpretation of Metaphysics Λ 10.
Glaucon's Question Ignored: Republic 519a-521b
Authors: Butler James
Published: May 2019

At Republic 519a-521b, Socrates claims that each guardian  must return from his/her contemplation to run Kallipolis. Quite reasonably, Glaucon objects that they would be making the guardian's life worse than it could be. This is sometimes referred to as “the happy philosopher problem”. But rather than answering Glaucon, Socrates admonishes him that their focus is instead on the role of the class of guardians and the happiness of the whole city. It turns out this admonition is the last in a string of similar admonitions that Socrates gives to his interlocutors. This paper examines Socrates' admonition to Glaucon, and its relation to Socrates’ other warnings  to focus on the happiness of the city. By examining these admonitions, we can defend Socrates' dismissal of Glaucon's question and the happy philosopher question at 519d. The paper concludes by examining a few strategies for interpreting Socrates’ reluctance to engage Glaucon’s question.
NET1 Enhances Proliferation and Chemoresistance in Acute Lymphoblastic Leukemia Cells
Authors: Sun Hongbo , Zhang Zhifu , Luo Wei , Liu Junmin , Lou Ye , Xia Shengmei
Published: May 2019

Acute lymphoblastic leukemia (ALL) is the most prevalent of pediatric cancers. Neuroepithelial cell-transforming 1 (NET1) has been associated with malignancy in a number of cancers, but the role of NET1 in ALL development is unclear. In the present study, we investigated the effect
of NET1 gene in ALL cell proliferation and chemoresistance. We analyzed GEO microarray data comparing bone marrow expression profiles of pediatric B-cell ALL samples and those of age-matched controls. MTT and colony formation assays were performed to analyze cell proliferation. ELISA assays,
Western blot analyses, and TUNEL staining were used to detect chemoresistance. We confirmed that NET1 was targeted by miR-206 using Western blot and luciferase reporter assays. We identified NET1 gene as one of the most significantly elevated genes in pediatric B-ALL. MTT and colony formation
assays demonstrated that NET1 overexpression increases B-ALL cell proliferation in Nalm-6 cells. ELISA assays, Western blot analyses, and TUNEL staining showed that NET1 contributes to ALL cell doxorubicin resistance, whereas NET1 inhibition reduces resistance. Using the TargetScan database,
we found that several microRNAs (miRNAs) were predicted to target NET1, including microRNA-206 (miR-206), which has been shown to regulate cancer development. To determine whether miR-206 targets NET1 in vitro, we transfected Nalm-6 cells with miR-206 or its inhibitor miR-206-in. Western blot
assays showed that miR-206 inhibits NET1 expression and miR-206-in increases NET1 expression. Luciferase assays using wild-type or mutant 3′-untranslated region (3′-UTR) of NET1 confirmed these findings. We ultimately found that miR-206 inhibits B-ALL cell proliferation and chemoresistance
induced by NET1. Taken together, our results provide the first evidence that NET1 enhances proliferation and chemoresistance in B-ALL cells and that miR-206 regulates these effects by targeting NET1. This study therefore not only contributes to a greater understanding of the molecular mechanisms
underlying B-ALL progression but also opens the possibility for developing curative interventions.
Changes in DNA Damage Repair Gene Expression and Cell Cycle Gene Expression Do Not Explain Radioresistance in Tamoxifen-Resistant Breast Cancer
Authors: Post Annemarie E. M. , Bussink Johan , Sweep Fred C. G. J. , Span Paul N.
Published: May 2019

Tamoxifen-induced radioresistance, reported in vitro, might pose a problem for patients who receive neoadjuvant tamoxifen treatment and subsequently receive radiotherapy after surgery. Previous studies suggested that DNA damage repair or cell cycle genes are involved, and could therefore
be targeted to preclude the occurrence of cross-resistance. We aimed to characterize the observed cross-resistance by investigating gene expression of DNA damage repair genes and cell cycle genes in estrogen receptor-positive MCF-7 breast cancer cells that were cultured to tamoxifen resistance.
RNA sequencing was performed, and expression of genes characteristic for several DNA damage repair pathways was investigated, as well as expression of genes involved in different phases of the cell cycle. The association of differentially expressed genes with outcome after radiotherapy was
assessed in silico in a large breast cancer cohort. None of the DNA damage repair pathways showed differential gene expression in tamoxifen-resistant cells compared to wild-type cells. Two DNA damage repair genes were more than two times upregulated (NEIL1 and EME2), and three
DNA damage repair genes were more than two times downregulated (PCNA, BRIP1, and BARD1). However, these were not associated with outcome after radiotherapy in the TCGA breast cancer cohort. Genes involved in G1, G1/S, G2, and G2/M
phases were lower expressed in tamoxifen-resistant cells compared to wild-type cells. Individual genes that were more than two times upregulated (MAPK13) or downregulated (E2F2, CKS2, GINS2, PCNA, MCM5, and EIF5A2) were not associated with response
to radiotherapy in the patient cohort investigated. We assessed the expression of DNA damage repair genes and cell cycle genes in tamoxifen-resistant breast cancer cells. Though several genes in both pathways were differentially expressed, these could not explain the cross-resistance for irradiation
in these cells, since no association to response to radiotherapy in the TCGA breast cancer cohort was found.
The Changing Role of Tourism Policy in Singapore's Cultural Development: From Explicit to Insidious
Authors: Ooi Can-Seng
Published: May 2019

In the last three decades, Singapore has transformed from a cultural desert to a global arts city, thanks significantly to tourism. The Singapore Tourism Board was proactively shaping the cultural dynamics and policy of Singapore until 2012. But since then its official role in the country's
arts and cultural development almost disappeared. The disappearance of tourism interests in cultural development stems apparently from years of resistance, dialogues, and negotiation. This study argues that the tourism authorities are still maintaining influence in the cultural dynamics and
development of Singapore by reframing its involvement. It insidiously asserts its influence by enticing members of the arts community with resources, opportunities, and economic support to participate in the tourism industry. This article provides a dialogical understanding of how tourism
has shaped Singapore's cultural dynamics. Cultural dynamics and tourism development in Singapore must be understood within economic and social engineering perimeters defined by the government. The tourism authorities do not only work with other government authorities, they use similar techniques
in managing and controlling cultural development in the city-state. The Bakhtinian Dialogic Imagination is the heuristic that organizes and structures the complex and dynamic tourism–culture relations in this study. Three dialogical concepts—carnivalesque, heteroglossia, and polyphony—are
used. Besides documenting the ongoing evolution of tourism in the cultural development of Singapore, this study questions the effectiveness of the arm's length approach to managing cultural development. The Singapore case shows that there are subtle economic and political ways to go round
that principle.
Accessible Charges in Structure-Activity Relationships. A Study on HEPT-based HIV-1 RT Inhibitors
Authors: Klein Christian Th. , Lawtrakul Luckhana , Hannongbua Supa , Wolschann Peter
Published: May 2019

The solvent accessibility of charges is introduced in QSAR studies. Atomic charges which do have contribution to the biological activity of a compound are more or less exposed to the environment (solvent), i.e. they have different possibilities to interact with biological macromolecules. Although one can imagine different ways in considering solvent accessibility, in this work it is taken into account by multiplying the net charge of an atom with its solvent accessible surface. To study the effect of accessibility of a charge on a biological activity, a large set (of 101) HEPT-based HIV- 1 reverse transcriptase (RT) inhibitors is analyzed, a molecu1a.r system, where the importance of electronic contribution is known. The results, based on multiple linear regression (MLR) and partial least squares (PLS) analysis, show that accessible charges correlate better with the RT inhibitory activity than net charges, leading to models with higher predictive ability.
Artificial Neural Networks in Drug Design 11: Influence of Learning Rate and Momentum Factor on the Predictive Ability
Authors: Kaiser D. , Tmej C. , Chiba P. , Schaper K.-J. , Ecker G.
Published: May 2019

A data set of 48 propafenone-type modulators of multidrug resistance was used to investigate the influence of learning rate and momentum factor on the predictive power of artificial neural networks of different architecture. Generally, small learning rates and medium sized momentum factors are preferred. Some of the networks showed higher cross validated Q2 values than the corresponding linear model (0.87 vs. 0.83). Screening of a 158 compound virtual library identified several new lead compounds with activities in the nanomolar range.
2-Amino-5,6-dihydro-1,4-benzochinon-Derivate
Authors: Kallmayer H.-J. , Doerr D.
Published: May 2019

The Diels-Alder-adducts 16A/B from 1,4-chlor-/1,4-bromanil (13A/B) and cyclopentadiene react with amines 8 to give the corresponding 6-amino-7-chloro-/bromo-quinones 17A/B. 2,6,6-Trimethyl-cyclohex-2-en-1,4-dion (5) and the non methylated Diels-Alder-adduct 11 from 1,4-benzoquinone and cyclopentadiene do not react as dihydroquinones with amines 8.
Die Reaktion des 2,3,4a,8a-Tetrachlor-6,7-dimethyl-4a,5,8,8a-tetrahydro-1,4-naphthochinons mit Aminen
Authors: Kallmayer H.-J. , Doerr M.
Published: May 2019

2,3,4a,8a-Tetrachloro-6,7-dimethyl-4a,5 ,8,8a-tetrahydro-1,4-naphthoquinone (5) reacts with arylamines 8a-e to give 2-amino-dihydroquinones 4a-e. Alkylamines 8f and h give 2-amino-dihydroquinones 4f, h and 2-amino-1,4-naphthoquinones 7f, h, dialkylamines 9f, g, i and j give 2-amino-dihydroqulnones 3f, g, i, j, 2-amino-1,4-naphthoquinones 6f, g, i, j and the photodesalkylated products 10f and g.
Synthesis and Anticalcium Activity of New Compounds Containing the 2,3-Dihydro-1,4-dioxino[2,3-b]pyridine System
Authors: Sánchez I. , Pujol MD. , Guillaumet G. , Massingham R. , Monteil A. , Dureng G. , Winslow E.
Published: May 2019

Summary: New compounds (3 and 4) possesing the 2,3-dihydro-1,4-dioxino[2,3-b]pyridine group were synthesized and tested as calcium antagonist agents. Both of them showed moderate anticalcium activity.
UNTERSUCHUNGEN ÜBER DIE NORDOST - ANATOLISCHEN FLECHTEN LOBARIA-SCROBICULATA UND L. PULMONARIA
Authors: Zeybek U. , Yıldız A.
Published: May 2019

The secondary metabolites in Lobaria pulmonaria and L. scrobiculata collected in northeast Anatolia are studied using HPLC. Constictic, nortictic and stictic acids are the major components in L. pulmonaria; in addition connorstictic, cryptostictic, and menegazziaic acids are present as minor constituents. In L. scrobiculata constictic, stictic, and usnic acids and m- scrobiculin are the major compounds; while cryptostictic and norstictic acids, and p- scrobiculin are present as minors.
Seasonal Depending Variations of the Composition and Biological Activities of Douglas Fir (Pseudotsuga menziesii) Essential Oils from Bulgaria
Authors: Jirovetz Leopold , Buchbauer Gerhard , Stoyanova Albena , Metodiev Stoyan
Published: May 2019

The seasonal depending variations of the essential oils of the needles with twigs of Bulgarian Douglas fir (Pseudotsuga menziesii, Pinaceae) were analyzed by GC-FID, GC-MS and olfactoric evaluation. In totally 8 investigated essential P. menziesii oils about 60 compounds could be identified with monoterpenes (especially sabinene and β-pinene) as main constituents. The antimicrobial effects against bacteria, fungi and worms of these volatiles as well as their olfactoric properties will be discussed.
SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW SULPHONAMIDES OF PYRIMIDINE
Authors: Cieplik Jerzy , Pluta Janusz , Gubrynowicz Olaf
Published: May 2019

The paper presents the synthesis of 5-substituted pyrimidine sulphonamides as well as the results of studies on the antibacterial and antifungal activity of obtained derivatives.
Atomic Absorption Spectrometry of Acidic Pharmaceutical Constituents by Precipitation Using Co (II), Cd (II) and Mn (II)
Authors: Salem Hesham , El-Maamli Magda , Shalaby Abdalla
Published: May 2019

Simple and accurate methods are described for the quantitative determination of flufenamic acid, mefenamic acid and tranexamic acid utilizing precipitation reactions with cobalt, cadmium and manganese. The acidic drugs were precipitated from their neutral alcoholic solutions with cobalt sulphate, cadmium nitrate or manganese chloride standard solutions followed by direct determination of the ions in the precipitate or indirect determination of the ions in the filtrate by atomic absorption spectroscopy. The optimum conditions for precipitation were carefully studied. The molar ratio of the reactants was ascertained. Statistical analysis of the results compared to the results of the official methods revealed equal precision and accuracy. The suggested procedures were applied for determining flufenamic acid, mefenamic acid and tranexamic acid in pharmaceutical preperations as well and proved validity.
Synthesis of Thienopyridines and Isoquinolines from 6-Amino-1,2-dihydro-4-methyl-2-thioxopyridine-3,5-dicarbonitrile and of Phthalazines from Thieno[3,4-c]pyridazine
Authors: Issac Y. A. , Ali M. S. , Erian A. W.
Published: May 2019

Thienopyridine 1 and thienopyridazine 13 have been readily reacted with electron-poor olefins to give isoquinolines and phthalazines, respectively. Some of the obtained compounds were tested for their antimicrobial activity.
Bufadienolides from Drimia robusta BAK
Authors: Krenn L. , Stapf V. , Kopp B.
Published: May 2019

From bulbs of Drimia robusta 7 bufadienolides were isolated, 3 of them new natural compounds. Structure elucidation was performed by comparison with authentic substances or by means of 1H-, 13C-NMR-spectroscopy and FAB-MS. The substances were identified as scilliroside (1), 12ß-hydroxyscillirosidin (2), 12ß-hydroxyscilliroside (3), hellebrigenin-3-0-ß-glucoside (4), 16ß-hydroxyhellebrigenin (5), 16ß-hydroxyhellebrigenin-3-O-ß-glucoside (6) and 5ß,16ß-dihydroxybufalin-3-O-ß-glucoside (7).
Buchariate: An Aromatic Ester from Salvia bucharica
Authors: Ahmad V. U. , Zahid M. , Ali M. S. , Ahmad S. , Ali Z. , Iqbal M. Z. , Tareen R.B.
Published: May 2019

Salvia bucharica belonging to the family Lamiaceae (Labiatae), afforded a new aromatic ester named buchariate [1-(p-hydroxybenzoyloxy)-3-oxo-octane (1)] along with twelve known constituents for the first time from our investigated source. The structures of all the isolated constituents were determined through spectroscopic techniques and comparison with literature values. The structure of new constituent (1) was elucidated through extensive 2-D NMR experiments.
Synthesis of Dioxigenated Systems. Preparation of Homologues of 1,4-Benzodioxin as Calcium Antagonists
Authors: Sánchez I. , Pujol M. , Guillaument G. , Massingham R. , Monteil A.
Published: May 2019

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.
Synthesis and In Vitro Evaluation of Chitosan-Thioglycolic Acid Conjugates
Authors: Bernkop-Schnürch Andreas , Hopf Thorid
Published: May 2019

The cationic thiomer chitosan-thioglycolic acid (TGA) shows excellent mucoadhesive features. In order to deepen the knowledge concerning this new excipient the optimization of its synthesis and a detailed characterization of its properties was the objective of this study Mediated by increasing quantities of a carbodiimide, thioglycolic acid was covalently attached to chitosan forming amide bonds with the primary amino groups of the polymer Determined with Ellman's reagent, 38 ± 3, 104 ± 2, 685 ± 43, and 885 ± 7 pmol thiol groups (n=3; ± SD) were bound per gram polymer at carbodiimide concentrations of 50, 75, 100, and 125 mM, respectively. The immobilized thiol groups displayed a comparatively higher reactivity to form disulfide bonds than the thiol groups in a corresponding mixture of chitosan and free unconjugated TGA. In an aqueous 0.5% (rnlv) chitosan-TGA gel 59 ± 5% of the thiol groups formed disulfide bonds within 6 hours at pH 6.0, whereas merely 5 ± 3% were oxidized in the corresponding physical mixture of chitosan and TGA. Diffusion studies showed that the modified polymer was capable of binding cysteine and cysteine methyl ester. The result supports the theory that the improved mucoadhesive properties of thiolated chitosan are based on the formation of disulfide bonds with cysteine moieties of mucus glycoproteins. Because of its availability via an efficient synthetic pathway and its mucoadhesive properties based on the capability to bind cysteine subunits, chitosan-TGA seems to be a promising new excipient for various drug delivery systems.
Extractive Spectrophotometric Determination of Nortriptyline Hydrochloride Using Sudan II, IV and Black B
Authors: Amin A. , Saleh H.
Published: May 2019

A simple spectrophotometric methods has been developed for the determination of nortriptyline hydrochloride in pure and in pharmaceutical

formulations based on the formation of ion-pair complexes with sudun II (SII), sudan (IV) (SIV) and sudan black B (SBB). The selectivity of the method was improved through extraction with chloroform. The optimum conditions for complete extracted colour development were assessed. The absorbance measurements were made at 534, 596 and 649 nm for SII, SIV and SBB complexes, respectively. The calibration graph was linear in the ranges 0.5- 280. 0.5- 37.5 and 0.5 – 31.0 μg ml−1 of the drug usiny the same reagents, respectively. The precision of the procedure was checked by calculating the relative standard deviation of ten replicate determinations on 15 μg ml−1 of nortriptyline HCI and was found to be 1.7, 1.3 and 1.55% using SII, SIV, and SBB complexes, respectively. The molar absorptivity and Sandell sensitivity for each ion-pair were calculated. The proposed methods were successfully applied to the deterniination of pure nortriptyline HCI and in pharmaceutical formulations, and the results demonstrated that the method is equally accurate, precise and reproducible as the official method.
Zur Farbreaktion von Amiloridhydrochlorid Ph. Eur.
Authors: Görlitzerl Klaus , Huth Silke , Jones Peter , Gößnitzer Edith , Wendelin Winfried
Published: May 2019

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.
Utility of Nickel for Atomic Absorption Spectrophotometric Determination of Selected Acidic Drugs
Authors: Salem Hesham , Kelani Khadiga , Shalaby Abdalla
Published: May 2019

A simple and accurate method is described for the quantitative determination of flufenamic acid, mefenamic acid, tranexamic acid, furosemide, diclofenac sodium and thiaprofenic acid by precipitation reactions with nickel(II) followed by direct determination of the ions in the precipitate or indirect determination of the ions in the filtrate by atomic absorption spectroscopy. Statistical analysis of the results compared to assays used in pharmacopeas and the Amax. methods revealed equal precision and accuracy. Furthermore the assays were also applied for the determination of these drugs in pharmaceutical preparations.
Aufnahme ausgewählter Metalle in Kompartimente von Solanaceen
Authors: Riße D. , Lahl H. , Unterhalt B.
Published: May 2019

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.
Antinociceptive Activity of Vigabatrin in Mice After Prolonged Treatment: Possible Development of Tolerance
Authors: Raza Muhammad , Al-Shabanah Othman , El-Hadiyah Tariq , Al-Bekairi Abdullah , Qureshi Shoeb
Published: May 2019

We have evaluated vigabatrin (γ-vinyi-γ-aminobutyric acid), an irreversible inhibitor of γ-aminobutyric acid (GABA)-transarninase responsible for GABA degradation, for its effects on nociceptive response, changes in spontaneous locomotor activity and body temperature in mice after a prolonged treatment regimen. The mice received vigabatrin 0.26% w/v chronically in drinking water for 7, 14 and 21 days. Changes in locomotion, body temperature and nociception were recorded after 7, 14 and 21 days respectively in different groups. Also, possible withdrawal symptoms were determined up to three days after 7, 14 or 21 days of treatment. In another experiment the animals were given acutely, 250 mg/kg of vigabatrin by oral gavage and the changes in response to the said parameters were assessed 90 min after treatment. Acute treatment increased the latency in the hot-plate reaction time and a highly significant decline in locomotion and body temperature. In contrast to the acute treatment studies, there were essentially no effects of vigabatrin on nociception, locomotor activity or body temperature either on the last day of each treatment or upon withdrawal for the next consecutive three days. We conclude that the changes in nociception, locomotion and body temperature after acute treatment with vigabatrin are due to neuromediator interactions and a possible direct effect of GABA accumulation. After prolonged treatment tolerance to the pharmacological effects of vigabatrin develop that was evident by no change in nociception, locomotion and body temperature. This may be attributed to the possible failure in the maintenance of GABA pools resulting in a reduction in enhanced GABA release mediated by vigabatrin in acute treatment. Further studies of mechanisms by which vigabatrin tolerance develops to these pharmacological responses are warranted.
Theoretical and Practical Considerations of the Newer Methods of the European Pharmacopeia for the Assay of Halide Salts of Organic Bases
Authors: Ragnar Bye
Published: May 2019

A certain type of titration methods have appeared with an increasing frequency during the last years, this being evident surveying the latest editions of the European Pharmacopeia (1997-2001) [1-3], where there are now more than fifty monographs on the assay of halide salt of organic bases by potentiometric titration of the sample dissolved in ethanol or in an ethanolwater mixture with sodium hydroxide after addition of a defined volume of diluted hydrochloric acid [...]
Effect of prolonged vigabatrin treatment on hematological and biochemical parameters in plasma, liver and kidney of Swiss albino mice
Authors: M Raza , OA Al-Shabanah , TM El-Hadiyah , AA Al-Majed
Published: May 2019

We have evaluated vigabatrin (γ-vinyl γ-aminobutyric acid), an irreversible inhibitor of γ-aminobutyric acid (GABA)-transaminase responsible for GABA degradation, for its effects on food consumption, body weight changes, fluid intake, changes in hematological and biochemical parameters in plasma liver and kidney of Swiss albino mice. Mice received vigabatrin 0.26% wlv chronically in drinking water for 7, 14 and 21 days. Changes in all the parameters were recorded aRer 7, 14 and 21 days respectively in different groups. Food consumption was comparable to the control group with minor fluctuations. The body weight declined significantly but only after 3-week treatment with no appreciable change in organ indices or relative organ indices. There were essentially no adverse effects on hematological parameters (RBC, WBC, HGB, neutrophils, eosinophils, monocytes, lymphocytes and basophils) with this treatment. However, there was a decrease in monocyte counts during the first week and an increase in the neutrophil counts during the third week of vigabatrin treatment. In one part plasma biochemical parameters like AST, ALT, CK-MB, creatinine, glucose and urea were also assessed with the same dose regimen. It was observed that only CK-MB and GPT activity levels were altered slightly significantly and are thought to be a result of cross enzyme inhibitions. In this experiment it was observed that lipid peroxide levels measured, as malondialdehyde did not change appreciably in both liver and kidney tissues. However, the levels of glutathione (non-protein sulfhydryl; GSH) declined significantly in comparison to control in liver and kidney. A comparison of level of GSH in liver and kidney shows that this depletion was at early time points in the former. The depletion of GSH suggests the possible involvement of GSH in detoxification process and corroborates its role in protection.
SYTHESIS AND ANTIBACTERIAL PROPERTIES OF PYRIMIDOPYRIMIDINES
Authors: Jerzy Cieplik , Janusz Pluta , Olaf Gubrynowicz
Published: May 2019

Our earlier works on synthesis and biological properties of the pyrimidine ring indicated that this system is extremely biologically active [...]
Spectrophotometric Determination of Trimebutine Through Ion- Pair and Charge- Transfer Complexation Reactions
Authors: Shaban M. Khalil
Published: May 2019

Summary Two simple and sensitive spectrophotometric methods are described for the assay of trimebutine. The first method is based on the interaction of the basic drug in 1,2 dichloroethane with bromocresol green (BCG); bromophenol blue (BPB) and bromothymol blue (BTB) in the same solvent to produce a stable yellow ion-pair complexes , which absorbed at 410,406 and 405nm, respectively. The second method is based upon the interaction of the basic drug with iodine in 1,2 dichloroethane. The yellow colour formed due to the formation of charge-transfer complex showed two maxima absorbed at 292 and 362 nm. Beer's law obeyed for both methods and the relative standard deviations were found to be less than 1 %. The two methods can be applied to the analysis of tablets, with no evidence of interference from excipients. A more detailed investigation on the complex was made to its composition, association constant and free energy change.
1-(4-Biphenylyl)ethylnitramine, bioisostere Profene
Authors: B. Unterhalt , T. Adam
Published: May 2019

Substituted 1-( 4-biphenylyl)ethylnitramines are synthesized from the 1-( 4-biphenylyl)ethanols 1a-d with ethyl N-nitro-carbamate in a Mitsunobu reaction [...]
Determination of Amineptine and Amprolium Hydrochlorides through Ion Associates with Cobalt (II) Thiocyanate
Authors: Fekria M. Abou Attia
Published: May 2019

Two new methods for the determination of amineptine (AMN) and amprolium (AMP) have been developed. The methods consist of extractin the ion - pairs between the drug and the inorganic complex [Co (SCN)4]−2. The optimal experimental conditions of both methods including pH, concentration of Co (II) and tlxocyanate ions, and the organic solvents were studied. The optimum pH was found to be 3.9, nitrobenzene proved to be the most suitable solvent, giving quantitative extraction for the two drugs. The two drugs can be determined in the organic phase spectrophotometrically at 625 nm showing Sandell sensitivities of 0.19 and 0.12 µg cm−2 with relative standard deviation of 0.46 and 0.87 % for amineptine and amprolium, respectively.The indirect method was also applied to measure cobalt in the organic phase by atomic absorption spectrometry at 240.7 nm, and the relative standard deviation of the method is approximately 0.35 and 0.29 % for amineptine and amprolium, respectively. The proposed methods were found to be suitable for the accurate, simple and rapid analysis of amineptine and amprolium hydrochlorides in the bulk drugs and in pharmaceutical forms.
The content of terpinen-4-01 in the essential oil of separate leaves and in hvdrodistilled oil of leaves and terminal twiqs of Juniperus communis L. var. saxatilis Pall.
Authors: Karlsen Jan , Svendsen Anders
Published: May 2019

Investigations with solid sampling gaschromatography of separate leaves and of hydrodistilled oil of Juniperus communis L. var. saxatilis Pall. growing in Norway at an altitude of 1000-1300 m above sea level, showed a terpinen-4-ol content varying from traces to about 1 % in separate leaves and up to 16-17% in hydrodistilled oil of uncomminuted leaves and twigs.
Abstracts of the Plenary Lectures, Short Lectures and Posters of the 17" Scientific Congress of the Austrian Pharmaceutical Society April 24 to April 26, 2003, Graz
Authors:   Osterreichische Pharmazeutische Gesellschaft
Published: May 2019

The uptake of Pb, Cd, Cu, Zn into the leaves and roots of Datura stramonium and Hyoscyamus niger. [...]
Svnthesis of 3-(3.5-Dioxo-[1,2,4]-oxadiazolidin-2-vl)propylphosphonic Acids
Authors: Kurz Thomas , Geffken Detlef , Wackendorff Claudia
Published: May 2019

Cyclic carbonylation of hydroxyureas 3 with 1,1'-carbonyldiimidazole gave 3-(3,5-dioxo-[1,2,4]oxadiazolidin-2yl)propylphosphonic acid diethyl esters 4 which were converted into the corresponding phosphonic acids 5 with bromotrimethylsilane.
Pyrrolizidine Alkaloids from Ligularia sibirica Cass. and Tephroseris integrifolia L.
Authors: Wiedenfeld Helmut , Narantuya S. , Dumaa M. , Monhbaatar A.
Published: May 2019

Tussilagine, isotussilagine, neo-tussilagine and neo-isotussilagine were isolated from Ligularia sibirica whereas Tephroseris integrifolia was found to contain senkirkine, otosenine, hydroxysenkirkine and 07-angeloylheliotridine. The structures were determined using spectroscopical methods (GC-MS; NMR).
Struktur und Eigenschaften des Benzidinblau-Chromophors N,N'-unsubstituierter Benzidine
Authors: Kallmayer H.-J. , Trojan B.
Published: May 2019

Die Benzidine A-E werden mit verschiedenen Oxidationsmitteln oxidiert und die entstehenden Benzidinblau-Chromophore isoliert. Spektrale Daten, Löseeigenschaften sowie die Farbigkeit und deren pH-Abhängigkeit charakterisieren die Benzidinblau-Chromophore als cr -Komplexe 7 und nicht als Radikalkationen 4.
Influence of Lipophilicity on the Antimycobacterial Activity of the Hydrochlorides of Piperidinylethyl Esters of Ortho-Substituted Phenylcarbamic Acids
Authors: Waisser K. , Dražková K. , Čižmárik J. , Kaustová J.
Published: May 2019

A series of 14 hydrochlorides of piperidinylethyl esters of orthosubstituted phenylcarbamic acids were evaluated for in vitro antimycobacterial activity against the strains of Mycobacterium tuberculosis, Mycobactenum kansasii and Mycobactenum avium. In vitro antimycobacterial activrty becomes higher with increasing hydrophobicity of the substituents. The alkoxy group is not necessary in order for the basic ethyl esters of phenylcarbamic acids to display antimycobacterial activity.
Hiqh-Perfonnance Thin-Laver Chrornatoaraphv for the Determination of Certain Antihypertensive Mixtures
Authors: Salem Hesham
Published: May 2019

A new simple, precise, accurate and selective high-performance thin-layer chromatographic (HPTLC) method has been developed for the simultaneous deter-mination of five mixtures: atenolol and chlorthalidone (Mix. l), enalapril maleate and hydrochlorothiazide (Mix. ll), amiloride hydrochloride and hydrochlorothiazide (Mix. lll), atenolol, chlorthalidone and amiloride hydrochloride (Mix. lV) and atenolol, hydrochlorottriazide and amiloride hydrochloride (Mix. V) in bulk powders and in pharmaceutical dosage forms. The methods consist of dissolving the drugs in methanol and spotting these solutions on a thin layer Merck HPTLC plates (0.25 mm thickness) pre-coated wrth 60 GF254 silica gel on aluminum sheet as the stationary phase, using dioxane:acetonrtrile: 1-propanol:hexane (30:18:23:1; v/v/v/v) , ethylacetate:chlo-roform:methanol:acetic acid (11:8:7.5:1.5; v/v/v/v). ethylacetate:chloroform:1-propanol:25% ammonia solution (12:9:1:0.2; v/v/v/v), di0xan:acetonitrile:1-propanol:tetrahydrofuran (20:13:4:15; v/v/v/v) and dioxane:ethylacetate:acetonitrile:1-propanol (10:7:5.5:3 v/v/v/v) as the mobile phases for mixtures l, ll, lll, lV and V, respectively. Detection was carried out densitometrically using UV detector at 283, 266, 257, 226 and 362 for atenolol, chlorthalidone, enalapril maleate, hydrochlorothiazide and amiloride hydrochloride, respectively. Calibration curves were linear in the range 1–100 µg/ml−1 with correlation coefficients not less than 0.9996. The percentage recoveries ranged from 98.3 ± 1.42 to 100.8 ± 0.79.
A VALIDATED HPLC-ASSAY FOR THE DETERMINATION OF MELOXICAM IN PRESENCE OF ITS DEGRADATION PRODUCTS
Authors: Bartsch Herbert , Eiper Angelika , Kopelent-Frank Hannelore , Procházka Jiři
Published: May 2019

The stability of aqueous solutions of meloxicam is studied with samples of different concentrations, and in different containers. Quantitation is carried out utilizing a validated stability indicating HPLC assay with five-point calibration. 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. A distinct correlation of the photodegradation rate with the concentration of the sample solution was found. Furthermore, the influence of size and geometry of the containers in which the solutions were exposed to light was investigated and results compared.
Effect of Granules Properties on the In-vitro and In-vivo Performance of Ibuprofen Sustained Release Matrix Tablets
Authors: Shubair M. S.
Published: May 2019

The impact of variations in the wet granulation step during the manufacturing process on the in-vitro and in-vivo performance of ibuprofen sustained release matrix tablets was investigated. Two batches were produced under different wet granulation conditions. The granules of the first batch (T1) were characterized by having a lower bulk density (0.56 g/ml), a higher percentage of fines (56.7% w/w) and a smaller geometric mean diameter (dg), 600 µm. While the granules of batch (T2) were characterized by having a more coherent properties, a higher bulk density (0.66 g/ml), a lower percentage of fines (36.9% w/w) and a larger dg, 720 µm. Three large scale production batches (B1, B2, B3) were manufactured similarly to T2 and found to have granules possessing similar properties. In-vitro tests showed that tablets of T1 had a statistically significant higher release rate constant than tablets of either T2, B1 ,B2 or B3. In-vivo tests were done using T1 and T2 tablets. Although T1 and T2 were bioequivalent with respect to Cmax and AUC, T2 exhibited a statistically significant longer sustained release characteristics than T1 (P<0.05).
In Vitro Evaluation of Sustained Released Matrix Tablet Formulations of Clarithromvcin
Authors: Genç Lütfi , Kıran A.
Published: May 2019

Sustained release matrix tablets of clarithromycin were prepared using different polymers as Hydroxypropyl methylcellulose (H PMC), Carbopol 934 and Eudragit RL/PO by direct compression technique. For the quality control of these formulations, weight deviation, hardness, friability, diameter-height ratio, content uniformity of the active substance and in vitro dissolution technique were performed. HPLC was used for the assay of clarithromycin and the assay method was validated. Dissolution profiles of the tablets were plotted and evaluated kinetically. The effects on drug release of polymer type and concentrations were investigated by 23 factorial design. The tablets containing HPMC, Carbopol 934 and Eudragit RLIPO were found suitably to sustain drug release
Completion of the Spectroscopical Data for the Synthesis of DIMBOA
Authors: Handler Norbert , Erker Thomas
Published: May 2019

Cyclic hydroxamic acids like 2,4-dihydroxy-7-methoxy-2H-1 ,4-benzoxazin-3(4H)-one (DIM BOA) and 2,4-dihydroxy-2H-1 ,4-benzoxazin-3(4H)-one (DIBOA) are found in several plants playing an important role in the defense-system of plants against a variety of enemies. To investigate new mechanism and effects we synthesized the molecules using known synthetic pathways. Since the chemical data of DIMBOA are not complete or even false, we decided to publish the missing ones in this journal.
The Synthesis and Bioloqical Properties of a 1-(2-Methylpyridin-4-yl) Olivacine Derivative
Authors: Jasztold-Howorko Ryszard , Doroszkiewicz Włodzimierz , Bugla-Płoskońska Gabriela , Croisy Alain , Carrez Daniele
Published: May 2019

Starting from 2-(6-methoxy-1-methyl-9H-carbazol-2-yl)ethylamine and 2-methylisonicotinic acid, 9-hydroxy-5,6-dimethyl-1-(2-methylpyridin-4-yl)-6H-pyrido[4,3-b]carbazole (5) was obtained. The new compound showed significant cytostatic activity for cultured L1210 cells and no inhibition of growth of the E. coli O56 strain was observed. The bactericidal activity of normal human serum against E. coli O56 was not affected by the examined compound 5 and its isomer 4.
Synthesis and Antidepressant Activity of Some New Coumarin Derivatives
Authors: Abdel-Latif Nehad A.
Published: May 2019

The coumarin-3-cinnamoyl derivatives 2a-d were prepared via Claisen-Schmidt condensation of 3-acetylcoumarin 1 with different aromatic aldehydes. Cycloaddition reaction of 2b,e with guanidine and thiourea yielded the corresponding aminopyrmimidine 3a,b and thioxypyrimidine derivatives 4a,b, respectively. Compounds 4a,b were condensed with chloroacetic acid or 3-bromopropionic acid to yield coumarin 3-thiazolo-pyrimidine 5a,b and thiazinopyrimidine 6a,b derivatives, respectively. Compounds 4a,b were condensed with chloroacetic acid and aromatic aldehyde to yield the aryl methylene derivatives 7a,b which could be prepared directly by condensation of compounds 5a,b with aromatic aldehydes. Compounds 2a-e were condensed with malononitrile or ethyl cyano acetate in presence of ammonium acetate to yield cyanopyridine 8a,b and cyanopyridone 9a-d derivatives, respectively, which were prepared by condensation of 3-acetylcoumarin 1, malononitrile or ethylcyanoacetate and aromatic aldehydes in presence of ammonium acetate. Condensation of compounds 2a,b,e with o-phenylenediamine in refluxing ethanol led to the formation of 10a-c as intermediate, followed by cleavage by thermolysis to benzimidazole derivative 11 along with compounds 12a-c as mixture, which were obtained directly by fusion of a,&unsaturated ketones 2 with ophenylene diamine at 200-220°C, while compound 11 could be prepared in pure form by fusion of 1 with o-phenylene diamine at the same temperature. The pharmacological screening showed that many of these obtained compounds have good antidepressant activity comparable to Tranylcypromine® as reference drugs.
Measuring internal auditor’s intention to blow the whistle (a Quasi-experiment of internal auditors in the local government)
Authors: Habbe Abdul Hamid , Rasyid Syarifuddin , Arif Hermita , Muda Iskandar
Published: May 2019

This study measures the cognitive moral development and tests its interaction with antecedent variables of prosocial behaviour such as fraud level, the status of person committing fraud and cohesiveness in affecting the willingness of internal auditors of local government (APIPs) to be a whistleblower. Quasi-experiment between subject design using pattern of 3×2×2×2 and 2×2 full factorial was employed in this research. The participants involved were internal auditors of 24 local governments in South Sulawesi which were divided into 18 groups. The data were analysed using ANOVA and t-test. The results of this study showed that based on the Cognitive Moral Development (CMD), majority of the internal auditors were categorised as pragmatic, the least number were autonomous, while accommodation was in between of both. Moreover, the intention of APIP to whistleblow was found high though insignificantly different among the three categories of CMD. Similarly, the different was insignificant among the variance of fraud level, the status of person committing fraud, and cohesiveness. The interaction between CMD and treatment variables resulted insignificant figure, except for the interaction between CMD and the fraud level which indicated significant result. Generally, it can be concluded that APIPs have a high intention to blow, but the intention will differ when their CMD interact with the fraud level and cohesiveness.
Dynamical Constraints on Mercury’s Collisional Origin
Authors: Clement Matthew S. , Kaib Nathan A. , Chambers John E.
Published: May 2019

Of the solar system’s four terrestrial planets, the origin of Mercury is perhaps the most mysterious. Modern numerical simulations designed to model the dynamics of terrestrial planet formation systematically fail to replicate Mercury, which possesses just 5% of the mass of Earth and the highest orbital eccentricity and inclination among the planets. However, Mercury’s large iron-rich core and low volatile inventory stand out among the inner planets, and seem to imply a violent collisional origin. Because most algorithms used for simulating terrestrial accretion do not consider the effects of collisional fragmentation, it has been difficult to test these collisional hypotheses within the larger context of planet formation. Here, we analyze a large suite of terrestrial accretion models that account for the fragmentation of colliding bodies. We find that planets with core mass fractions boosted as a result of repeated hit-and-run collisions are produced in 90% of our simulations. While many of these planets are similar to Mercury in mass, they rarely lie on Mercury-like orbits. Furthermore, we perform an additional batch of simulations designed to specifically test the single giant impact origin scenario. We find less than a 1% probability of simultaneously replicating the Mercury–Venus dynamical spacing and the terrestrial system’s degree of orbital excitation after such an event. While dynamical models have made great strides in understanding Mars’ low mass, their inability to form accurate Mercury analogs remains a glaring problem.