bluuebunny/crossref_metadata_2025 huggingface dataset:
A chemically contiguous hapten approach for a heroin–fentanyl vaccine
Authors: Natori Yoshihiro , Hwang Candy S , Lin Lucy , Smith Lauren C , Zhou Bin , Janda Kim D
Published: May 2019

Background: Increased death due to the opioid epidemic in the United States has necessitated the development of new strategies to treat addiction. Monoclonal antibodies and antidrug vaccines provide a tool that both aids addiction management and reduces the potential for overdose. Dual drug vaccines formulated by successive conjugation or by mixture have certain drawbacks. The current study examines an approach for combatting the dangers of fentanyl-laced heroin, by using a hapten with one epitope that has domains for both fentanyl and heroin.

Results: We evaluated a series of nine vaccines developed from chemically contiguous haptens composed of both heroin- and fentanyl-like domains. Analysis of the results obtained by SPR and ELISA revealed trends in antibody affinity and titers for heroin and fentanyl based on epitope size and linker location. In antinociception studies, the best performing vaccines offered comparable protection against heroin as our benchmark heroin vaccine, but exhibited attenuated protection against fentanyl compared to our fentanyl vaccine.

Conclusion: After thorough investigation of this strategy, we have identified key considerations for the development of a chemically contiguous heroin–fentanyl vaccine. Importantly, this is the first report of such a strategy in the opioid–drug–vaccine field.
Thieno[2,3-b)pyridinones as Antagonists on the Glycine Site of the N-methyl-ᴅ-aspartate Receptor - Binding Studies, Molecular Modeling and structure-Activity-Relationships
Authors: Buchstaller H.-P. , Siebert C.D. , Lyssy R.H. , Ecker G. , Krug M. , Berger M.L. , Gottschlic R. , Noe C.R.
Published: May 2019

Within the frame of the synthesis of glycine antagonists, a series of novel thieno[2,3- b]pyridinones with substituted phenyl residues in position 5 were synthesised to investigate the importance of the torsion angle between the pyridinone skeleton and the phenyl ring for binding affinity. The parent compound, 4-hydroxy-5-phenylthieno[2,3-b]pyridine-6(7H)-one, and its thienyl analogue, exhibited highest potencies, whereas compounds with ortho-substituted aryl moieties in position 5 showed decreased activities. This seems to be due to unfavourable steric interactions and increased torsion angles between the thieno[2,3- b]pyridinone system and the aryl substituent in position 5. Further evidence is drawn by QSAR studies, which showed an inverse relationship between the size of the ortho-substituent and the binding affinity.
A Simple Kinetic Spectrophotometric Method For The Determination of Certain 4-Quinolones in Drug Formulations.
Authors: Rizk M. , Belal F. , Ibrahim F. , Ahmed S. M. , El-Enany N. M.
Published: May 2019

An accurate simple and selective kinetic procedure for the determination of certain 4-quinolones namely, norfloxacin (I), ofloxacin (II), enrofloxacin (III), fleroxacin (IV), ciprofloxacin (V) and pefloxacin (VI) is described. The procedure is based on reacting the studied compounds in acidic media (0.1 M HCL) with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in presence of cerium (IV) ammonium sulphate as an oxidant at room temperature for a fixed time of 20 min. for (I), (III), 12 min for (II) and 30 min for IV , V and VI, then the absorbance of the reaction product is measured at 630 nm. The concentration of the studied compounds is computed using the corresponding calibration curve equation for the fixed-time method. The absorbance-concentrations plot is rectilinear over the range 20-100 ug.ml-1 for (I), 2 - 20 ug.ml-1 for (II), 10 - 74 ug.ml-1 for (III), 10 - 60 ug.ml-1 for IV, 10 - 50 ug.ml-1 for IV and 8 - 40 ug.ml-1 for VI. The determination of the studied compounds by the fixed-concentration and rate constant methods is feasible with the calibration equation obtained, but the fixed-time method proved to be more applicable. The procedure was applied successfully to commercial tablets and ampoules and the results obtained were compared statistically with the reference methods.
Ion-pair Spectrophotometric Determination of Dibucaine
Authors: Shubietah Raqi M. , Zuhri Ali Z.Abu , Khalid Bashar A.
Published: May 2019

A simple and sensitive spectrophotometric determination of dibucain has been established. It is based on the formation of colored ion-pair complexes between Dibucaine and each of Orange II, Orange G, Bromothymol blue and Bromocresol green. The extract with each of the previous dyes in chloroform exhibited a specific wavelength of maximum absorbance, and all these wavelengths lied in the range 416 to 500 nm. The linear range extended from 1.5 to 60 ppm. The optimum conditions were selected after studying many variables such as pH, shaking time, temperature and dye concentrations. The method was also selective for the analyte and the drug excipients did not interfere.
Pharmacognostical examination concerning the hemostyptic effect of Achillea millefolium Aggregat
Authors: Sellerberg U. , Glasl H.
Published: May 2019

Yarrow (Achillea mille/olium Aggregat) is traditionally used against bleeding. Aqueous hot extracts were turbid and shortened the recalcification time, a global test ofthe blood coagulation. The residue obtained by membrane filtration of these extracts was the active fraction. This residue is problably located mostly in the stem. By pressure obtained juice elongated the blood coagulation. Compared with non-flowering and wilthed material, the blooming herb showed best effects. The storage conditions had no effect on the activity ofthe herb.
Pyrrolizidine Alkaloids in Senecio nemorensis L. from Mongolia
Authors: Wiedenfeld Helmut , S. Narantuya , D. Altanchimeg , Roeder Erhard
Published: May 2019

We isolated four Pyrrolizidine Alkaloids (PA) from Senecio nemorensis L. growing in Mongolia. Their structures were elucidated by spectroscopic methods to be 7-Senecioyl-9-sarracinoyl-retronecine, Retroisosenine, Doriasenine and Bulgarsenine. The alkaloidal pattern is very similar to that of the European Senecio nemorensis L., ssp. nemorensis (Rchb.) Celak. The medicinal use of this plant or of preparations from it may be hazardous to human health because of the high PA level in the plant (≈ 0.1%) and the fact that three of the PA are known to have toxic side-effects.
Analysis of the Essential Oil of the Aerial Parts of the Medicinal Plant Aristolochia indica Linn. (Aristolochiaceae) from South-India
Authors: Jirovetz Leopold , Buchbauer Gerhard , Puschmann Christiane , Fleischhacker Wilhelm , Shafi P.Mohamed , Rosamma M.K.
Published: May 2019

The essential oil of the aerial parts of Aristolochia indica Linn. (Anstolochiaceae) from South-India was analyzed by gas chromatographic-spectroscopic (GC-FID and GC-MS) and olfactoric methods to identify those compounds responsible for the characteristic odor as well as partly for the folk medicinal use of this plant. Especially sesqui- and monoterpenes were found to be dominating constituents of this essential oil, such as: β-caryophyllene, α-humulene, ishwarone, caryophyllene oxide I, ishwarol, ishwarane and aristolochene as well as linalool and α-terpinolene.The odor impression of the sample is described and the possible biological activity of some single volatiles shortly discussed.
6-, 7- AND 8-(5-ARY L-1-PHENYL-2-PYRAZOLIN-3-LY)IMIDAZO- AND PYRIMIDO[2,1-b]BENZOTHIAZOLES AS NOVEL ANTICONVULSANT AGENTS
Authors: Gineinah Magdy
Published: May 2019

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.
Analysis, Chemotype and Quality Control of the Essential Oil of a New Cultivated Basil (Ocimum basilicum L.) Plant from Bulgaria
Authors: Jirovetz Leopold , Buchbauer Gerhard , Stoyanova Albena , Balinova Anastasia
Published: May 2019

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.
Pyrocatechol Violet in Pharmaceutical Analysis Part II. A Spectrophotometric Method for the Determination of Paracetamol in Pure and in Pharmaceutical Dosage Forms
Authors: Amin Alaa
Published: May 2019

A spectrophotometric method for the selective determination of paracetamol based on its reaction with pyrochatechol violet under basic conditions to form an ion-pair complex is described. The absorption maximum of the coloured ion-pair formed is observed at 652 nm and the molar absorptivity is 4.54 x10-3l mol-1 cm-1. Beer's law is obeyed over the concentration range 0.5-34.0 μg ml-1, while that obtained using Ringbom method is in the range 3.5 -32.0 μg ml-1. There is no interference from common additives, excipients and commercial drugs present in their formulations suggesting a highly selective procedure compared with others. Statistical analysis of the obtained results showed that there is, no significant difference and absence of any systematic error in the method compared with the official one. The method is simple, rapid and convenient and was applied successfully to the determination of paracetamol in pure and in its dosage forms compared with the official method.
Synthese, Reaktivität und fungizide Eigenschaften von 4-Hydroxy(Alkoxy)iminooxazolidin-2-onen
Authors: Geffken Detlef , Riederer Cordula
Published: May 2019

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 beobtained in low yields. From the prepared novel compounds only 3a displayed a remarkable fungicidal activity at 2 ppm.
Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs
Authors: Abdel Hamid S. , El-Obeid H. , Al-Rashood K. , Khalil A. , El-Subbagh H.
Published: May 2019

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.
ALKALOIDS FROM OXYTROPIS MYRIOPHYLLA (PALL) DC
Authors: Kojima Keisuke , S. Purevsuren , S. Narantuya , S. Tsetsegmaa , Ya Jamyansan , Lsaka Kimio , Ogihara Yukio
Published: May 2019

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.
4th Central European Symposium on Pharmaceutical Technology / Oral presentations
Authors:   Osterreichische Pharmazeutische Gesellschaft
Published: May 2019

Intravesical instillation of a drug solution is a common way of treating urinary bladder infections and superficial bladder cancer. [...]
4th Central European Symposium on Pharmaceutical Technology / Poster presentations
Authors:   Osterreichische Pharmazeutische Gesellschaft
Published: May 2019

Using waxy materials, several controlled release tiaprofenic acid (TA) tablets were prepared. [...]
Influence of aminoacid anions on the absorption process of Mg2+ ions in vitro
Authors: W. Marcoin , B. Szulc
Published: May 2019

Influence of aminoacid anions on the absorption process of Mg2+ ions in vitro - The results of the research on influence of modification in the structure of magnesium salts with glycine on the process of Mg (11) ions absorption were presented in this paper. A flow-through apparatus containing a piece of small intestine of a rat was used for the absorption rate measurement of selected organic magnesium salts. The results of the investigations showed the positive influence of modification of the structure on the absorption process. A correlation was established between quantity of absorbed magnesium and the partition coefficient values (log P).
Spectrophotometric determination of some pharmaceutical piperazine derivatives by charge-transfer and ion-pair complexation methods
Authors: Y.M. Issa , F.M. Abou-Attia , F.M. Abdel-Gawad , S.M. Abdel-Hamid
Published: May 2019

Simple and sensitive spectropliotometric methods are described for the assay of three piperazine derivatives ketoconazole, trimetazidine hydrochloride and piribedil based on cliarge-transfer and ion-pair complexation reactions. The first method is based on the reaction of the basic drug with iodine as o-acceptor in dry 1,2-dichloroethane to form a yellow colour due to the formation of charge-transfer complex showing maximum absorbence at 363, 364 and 359 nm for ketoconazole, trimetazidine hydrochlorid and piribedil, respectively. The second method is based on the reaction of basic drug with bromocresol green (BCG) in dry 1,2- dichloroethane to form a stable yellow coloured complex with maximum absorbance at 407, 408 and 410 nm for ketoconazol, trimetazidine hydrochloride and piribedil, respectively. Beer's law was obeyed for both methods and the relative standard deviations were found to be less than 1%. The two methods can be applied for the analysis of tablets and cream, with no evidence of interference from excipients. A more detailed investigation of the complex was made with respect to its composition association constant and free energy cliange.
Atypisches Verhalten von Thiophenderivaten gegeniiber Reduktions- bzw. Thionierungs-Versuchen
Authors: Erker T. , Trinkl K.
Published: May 2019

To prepare required thiolactarns. initial experiments were done with the lactarns 1 - 3 and Lawessol reagent. However in preliminary trials. treatment of the compounds failed to give the desired molecules. Modification of the reaction conditions. paticularly with regard to the solvent and the reaction temperature. did not permit the preparation of the corresponding thiolactams. The keto function in position 6 was thought to be responsible for this atypical behaviour. Therefore. as the following step. the acetyl group in compounds 1 - 3 should be reduced to the corresponding ethyl derivatives. This reaction did not give the needed bicycles. Reduction of compounds 4 - 6 with triethylsilanel trifluoroacetic acid brought up compounds 7 - 9.
Composition and stability of complexes of Ephedrine hydrochloride with Ni2+, Zn2+, and Cd2+ as toxic ions
Authors: EL Guindi Nabawia
Published: May 2019

The complexes of Ephedrine with Nickel, Zinc and Cadmium ions have been investigated spectrophotometricalfy using the method of corresponding solutions [I-3] and pH-metrically using Irving and Rossoti technique [4] Two compositions were observed spectrophotometrically 1 : 1 and 2: 1 (L: M) for concentration of metal ions (0.5 x 10-3 M and 1 x 10-3 M) hile the first composition only predominate at concentration of metal ions (1.5 x 10-3 M and 2 x 10-3 M ). The stability of complexes show that complexes of Ni2+ are more stable than that of Zn2+ an Cd2+, Moreover, the composition and stabilities of complexes were studied pHmetrically in aqueous medium at 0.1 M NaCl and two different temperatures 30°C and 40°C; hence the value of the free energy change (ΔG°), the enthalpy (ΔH°) and the entropy (ΔS°) were calculated at 30°C. Beside the role of Ephedrine as chelating agent to toxic elements, the complexometric method was used for the determination of Ephedrine in its pure form and in tablets.
Lacking of efflux mechanism in clinical isolate of Pseudomonas aerupinosa highly resistant to β-Lactams And imimnem
Authors: Kadry Ashraf.
Published: May 2019

In this investigation, the isolate of Pseudomonas aeruginosa from cystic fibrosis was highly resistant to β-lactarns and β-lactamase inhibitors. The resistant determinants of clinical isolate to imipenem, ceftazidime, ceftriaxone and cefepime were conjugally non-transfer. The slow or non-enzymatically mediated breakdown of imipenem and other broad spectrum p-lactams suggest the resistance of P.aeruginosa isolate to these drugs might be attributed to either permeability or efflux. Impaired penetration of imipenem and other p-lactams through the membrane was detected by a diminished expression of outer membrane (OM) proteins of approximate weight of 46 and 39 Kdal, matched to Opr D and OprF, respectively. Efflux resistance mechanism for meropenem and p-lactams has been ruled out since the isolate failed to express outer membrane protein of about 50 Kdal, which is matched to Opr M protein channel. Thus, reduced permeability in the clinical isolate may be the main mechanism conferring resistance against p-lactarns including imipenem.
Quantitative determination of the faradiol esters in marigold flowers and extracts
Authors: Reznicek Gottfried , Zitterl-Eglseer Karin
Published: May 2019

An HPLC method is introduced for the precise quantitative determination of the anti-inflammatory active faradiol esters from marigold flowers and extracts. After a prepurification the HPLC analysis allows the proof of the quality of marigold flowers or C02-extracts used for pharmaceutical preparations.
Contribution to the Analysis of the Volatile Constituents from some Lavender and Lavandin Cultivars Grown in Greece
Authors: Chakopoulou Paschalina , Goliaris Apostolos , Katsiotis S.
Published: May 2019

The essential oils of Lavandula angustifolia and the Lavandin hybrids "super" and "special" grown in Greece, were studied in order to evaluate their quality as far as the correlation of their essential oil composition. The essential oil yields were determined to 4.4%, 7.5% and 8.5% in the lavandula and lavandin "super" and "special" hybrids respectively. Fifty-nine constituents were identiiied representing the 99% of the oils. The qualitative analysis of the oils was carried out by GCIMS and revealed that linalool and linalylacetate were the predominant constituents. Remarkable differences were noticed between the camphor percentages among them (11.35% and 5.03% for the "super " and "special" respectively).
Synthesis and Pharmacological Evaluation of Fenamate Analogues: 1,3,4-Oxadiazol-2-ones and 1,3,4-Oxadiazole-2-thiones
Authors: El-Azzouny Aida , Maklad Yousreya , Bartsch Herbert , Zaghary Wafaa , Ibrahim Waleed , Mohamed Mosaad
Published: May 2019

A series of fenamate pyridyl or quinolinyl analogues of 1,3,4-oxadiazol-2-ones 5a-d and 6a-r, and 1,3,4-oxadiazole-2-thiones 5e-g and 6s-v, respectively, have been synthesized and evaluated for their analgesic (hot-plate) , antiinflammatory (carrageenin induced rat's paw edema) and ulcerogenic effects as well as plasma prostaglandin E2 (PGE2) level. The highest analgesic activity was achieved with compound 5a (0.5 ,0.6 ,0.7 mrnolkg b.wt.) in respect with mefenamic acid (0.4 mmollkg b.wt.). Compounds 6h, 6l and 5g showed 93, 88 and 84% inhibition, respectively on the carrageenan-induced rat's paw edema at dose level of 0.1rnrnol/kg b.wt, compared with 58% inhibition of mefenamic acid (0.2mmoll kg b.wt.). Moreover, the highest inhibitory activity on plasma PGE2 level was displayed also with 6h, 6l and 5g (71, 70,68.5% respectively, 0.lmmolkg b.wt.) compared with indomethacin (60%, 0.01 mmolkg b.wt.) as a reference drug. In addition 6i, 6k, 6p, 6r, 6t and 6v were devoid of any ulcerogenicity.
Colourimetric and atomic absorption spectrometric determination of some f luoroquinolone derivatives
Authors: Salem Hesham
Published: May 2019

Three simple, accurate, sensitive and selective procedures for the determination of ten fluoroquinolones (amifloxacin, ciprofloxacin hydrochloride, difloxacin hydrochloride, enoxacin, enrofloxacin, lomefloxacin hydrochloride, lovefloxacin, norfloxacin, ofloxacin and pefloxacin mesylate) were described. Procedures I and II are based on the formation of ion-pair complexes between the drugs and ammonium reineckate reagent in an acidic medium at 25 ±2°C and the formed precipitates are quantitatively determined either colourimetrically (procedure I) or by atomic absorption spectrometrically (procedure II). Procedure I is based on dissolving the formed precipitate with acetone, the volume was completed quantitatively and the absorbance of the solution was measured at 527 nm against pure solvent blank. The formed precipitates on the atomic absorption spectrometric procedure (procedure II) are quantitatively determined either directly or indirectly through the chromium precipitate formed or the residual un-reacted chromium in the filtrate at 358.6 nm and the optimum conditions for precipitation have been carefully studied. Procedure Ill is based on the reaction of the studied drugs with 2,2-diphenyl-1-picrylhydrazyl reagent (DPPH). The latter is employed to abstract a hydrogen atom from the drugs thereby promoting a process of radical coupling. This results in a reduction of the violet color of DPPH with the formation of the yellow colored 2,2-diphenyl-1-picrylhydrazine (DPPH2). The decrease in the intensity of the violet color is used to measure the concentration of the drugs. All measurements are made at λ = 520 nm on methanolic solutions of the reagent and drugs. Beer's law is obeyed for the studied drugs in the range 2-36 µg ml−1 with correlation coefficients not less than 0.9992. All procedures hold well accuracy and precision when applied to the analysis of the cited fluoroquinolones in different dosage forms with good recovery percent ranged from 98.88±0.40 to 100.99±0.44 without interference from additives.
Abbauprodukte von Amiloridhydrochlorid
Authors: Görlitzer Klaus , Huth Silke , Gößnitzer Edith , Wendelin Winfried
Published: May 2019

Erhitzen von Amiloridhydrochlorid (1 • Hcl) in Acetatpuffer pH 4.6 führte zu Amiloridacetat (1 • AcOH), dem Pyrazindiamin 6 und dem Acylureid 7. Das Pteridinon 3 wurde beim Erhitzen von 1 • Hcl in DMF unter Rückfluß erhalten.
Synthesis and antimicrobial evaluation of 3-hydrazino-quinoxaline derivatives and their cyclic analoaues
Authors: EI-Bendary E. R. , Goda F. E. , Maarouf A. R. , Badria F. A.
Published: May 2019

A series of quinoxaline derivatives has been synthesized by reacting 3-hydrazinoquinoxalines 1a,b with many bifunctional reagents. Reaction of 1a,b with chloroacetyl chloride and ethyl chloroacetate afforded 1-chloromethyl[1,2,4]tnazoIo[4,3-a]quinoxalines 2a,b and dihydro[1,2,4]triazino[4,3-a]quinoxalin-2-ones 3a,b respectively. Condensation of 1a,b with ethyl acetoacetate and acetylacetone yielded 2-quinoxalinylhydrazonobutanoates 4a,b and 2-quinoxalinylhydrazono-2-pentanones 5a,b respectively. Cyclization of 5a,b gave 3,5-dimethylpyrazolylquinoxalines 6a,b. Moreover, reaction of compounds 2a,b with N-phenyl piperazine derivatives afforded 4-(4-Arylpiperazin-1-yl)-1-[(4-arylpiperazin-1-yl) methyl)]triazoloquinoxalines 7a−e. The prepared compounds were screened for in vitro antibacterial and antifungal activities. None of the tested compounds showed significant activity towards Pseudomonas aeruginosa. However, remarkable activities were noticed for compounds 5a and 5b against Eschenchia coli. Staphylococcus aureus and Candida albicans. Compounds 6a and 6b lacked any antimicrobial activities against the tested microorganisms.
Study of local anesthetics. Part* 166:Conductometric determination of the critical micelle concentration of local anesthetic heptacainium chloride in aqueous electrolvte solution
Authors: Andriamainty F. , Čižmárik J. , Holíková M.
Published: May 2019

Specific conductivities of local anesthetic heptacainium chloride XlX (HCC XlX) (N-[2-(2-heptyloxyphenylcarbamoyloxy)-ethyl]-piperidinium chloride), in aqueous electrolyte solution (0.05 mol.1−1 NaCl) were measured as a function of the concentration and temperature. The critical micelle concentrations (c.m.c) and the counterion (β) binding of the micelles were estimated from the dependence of the specific conductivity of the substrate concentration. The temperature dependence of ln c.m.c was fitted to the function of the second degree polynomial. From the fitting parameters, Gibss free energies (ΔG0), enthalpies (ΔH0), and entropies (ΔS0) of micellization as a function of temperature were estimated. The "mass action model" was applied to micelle formation to calculate the micellization parameters.
Comparative Bioavailabilitv Studv of Two Brands of Terbutaline Sulphate Tablets in Healthy Human Volunteers
Authors: Barakat Nahla S. , Khalafallah Nawal M. , Khalil Said A.
Published: May 2019

The purpose of this study was to evaluate the bioavailability of locally produced 2.5 mg terbutaline sulphate tablets (brand A ) relative to a reference product, Bricanyl 2.5 mg tablets (brand 6). The study was a single dose 5 mg randomized crossover one in 15 healthy volunteers in the fasting state. Urine was collected at intervals of 24 h. Total terbutaline excreted in urine as unchanged drug and as conjugates (sulphate and glucuronide) was determined by a developed and validated HPLC method. In-vitro characteristics of both brands were similar. Based on percent of the dose excreted in urine, the oral bioavailability ranged from 33.5% to 75.8% for both brands. Statistics were applied to judge bioequivalence according to USP 24 in-vivo bioequivalence guidance. Results indicated that brand A and B were bioequivalent and hence interchangeable in medical practice.
Differential Pulse Voltammetric Determination of Loperamide in a Pharmaceutical Dosaqe Form
Authors: Radi A. , Elmogy T.
Published: May 2019

A voltammetric study of the oxidation of loperamide has been carried out at the glassy carbon electrode. This compound exhibited a single peak in Britton-Robinson buffer solutions of pH 5.0–11.0, with a maximum current at pH 8.0. The electrochemical oxidation of loperamide is identified as an irreversible, diffusion-controlled process. Based on this study, a simple, rapid and sensitive voltammetric method was applied, without any interference from the excipients, to the determination of the drug in a capsule dosage form.
Effect of hydrophilic substances on liberation of quinidine from starch—methylcellulose spheres
Authors: Kasperek Regina , Czarnecki Wiktor
Published: May 2019

The spheres were prepared by the desolvation technique combined with gravitational sedimentation of droplets of methylcellulose gel suspensions with the addition of 25% quinidine adsorbate on the potato starch and 5% hydrophilic agents such as Span 80, Tween 60, glyceryl monostearate or PEG 2000 instilled into a desolvation liquid (saturated sodium acetate:paraffin liquid:heptane 1:1:1, v/v/v) through a standardized capillary.As follows from the physicochemical studies the sphericity (Sp) changed within the range 1.020–1.314, the porosity (P) was 19.1–66.5% and the loading efficiency was 35.10–67.07%. The release studies show that the dissolution efficiency after 60 min (DE60) in acidic medium was 78.6% for quinidine and 52.6–63.4% for the spheres; in phosphate buffer pH 6.8 DE60 was 32.4% for quinidine, but ranged within 16.3–26.0% for the spheres. The release of the drug from the spheres was fast and it was slightly difference (the loaded drug was released within 60 min) in acidic medium, while differentation of release in the phosphate buffer made it possible to evaluate the effect of hydrophilic additives on the dissolution rate.The general process of release can be described by the modified Higuchi equation Mt*=K0·(t−TD) , which facilitates the analysis of the theoretical amount of the released substance Mt* depending on the zero-order dissolution rate constant K0 and the dissolution lag time (TD). Accordingly, spheres with sustained release can be most effectively produced by addition of PEG 2000. These spheres are characterized by Sp = 1.035, P = 60.2% and a loading efficiency of quinidine 67.07%. The release in acidic medium proceeds with K0 = 3.857 mg·min−0.5 and TD = 6.21 min, in phosphate buffer K0 was 1.293 rng·min−0.5 and TD = 7.14 min. These parameters were of less importance for the other formulations. The modified Higuchi equation gives information about the parameters of drug released.
Study of Local Anesthetics. Part* 168 Critical Micelle Concentration of Alkyloxy Homoloqs of Local Anesthetic Heptacainium Chloride Determined by Ion Sensitive Electrode
Authors: A ndriamainty F. , Čižmárik J. , Uhríková D. , Balgavý P.
Published: May 2019

The critical micelle concentrations (c.m.c.) of alkyloxy homologs of local anesthetic N-[2-(2-alkyloxyphenylcarbamolyoxy)-ethyl]-piperidinium chloride (CnA) with n=3, 5, 7, 8, 10 and 12 carbons in alkyloxy substituent determined by surfactant ion sensitive electrode (ISE) depend exponentially on n: lnc.m.c.=0.70+0.49n and lnc.m.c.=0.57+0.62n at t=25 °C and pH≈4.5 in water and 0.1 mol.l-1 NaCl solution, respectively, where the free energy of transfer of the alkyloxymethylene group from the aqueous phase into the micelle hydrophobic interior is ΔG0=(-0.49±0.008)RT in water and ΔG0=(-The critical micelle concentrations (c.m.c.) of alkyloxy homologs of local anesthetic N-[2-(2-alkyloxyphenylcarbamolyoxy)-ethyl]-piperidinium chloride (CnA) with n=3, 5, 7, 8, 10 and 12 carbons in alkyloxy substituent determined by surfactant ion sensitive electrode (ISE) depend exponentially on n: lnc.m.c.=0.70+0.49n and lnc.m.c.=0.57+0.62n at t=25 °C and pH≈4.5 in water and 0.1 mol.l-1 NaCl solution, respectively, where the free energy of transfer of the alkyloxymethylene group from the aqueous phase into the micelle hydrophobic interior is ΔG0=(-0.49±0.008)RT in water and ΔG0=(-0.62±0.06)RT in the 0.1 mol.l-1 NaCl solution. The enthalpic and entropic contributions to the standard Gibbs energy of micellization of heptacainium chloride (heptyloxy homologs of CnA) in 0.1 mol.l-1 NaCl solution were calculated according to the phase separation model in the temperature range of 25-45 °C.0.62±0.06)RT in the 0.1 mol.l-1 NaCl solution. The enthalpic and entropic contributions to the standard Gibbs energy of micellization of heptacainium chloride (heptyloxy homologs of CnA) in 0.1 mol.l-1 NaCl solution were calculated according to the phase separation model in the temperature range of 25-45 °C.
Antimicrobial testinas and gas chromatoaraphic analvsis of pure oxvaenated monoterpenes 1.8-cineole, α-terpineol, terpinen-4-ol and camphor as well as target comoounds in essential oils of pine (Pinus pinaster), rosemary (Rosmarinus officinalis), tea tree (Melaleuca alternifolia)
Authors: Jirovetz Leopold , Buchbauer Gerhard , Denkova Zapriana , Stoyanova Albena , Murgov Ivan , Schmidt Evrich , Geissler Margit
Published: May 2019

The oxygenated monoterpenes 1,8-cineole, α-terpineol, terpinen-4-ol and camphor as well as essential oils of pine, rosemary and tea tree, rich in these volatiles, were tested for their antimicrobial activities against some different strains of yeast, Gram-(-)- and Gram-(+)-bacteria by agar diffusion and agar dilution method, respectively. The same was done using the phenolic aroma compound eugenol as a reference-substance. The monoterpene alcohols a-terpineol and terpinen-4-ol were found to be active against all strains used in a wide range. The same result was obtained for the testings of essential oils of pine, rosemary (2 samples) and tea tree. Nearly all aroma chemicals and essential oils did show a significant high antimicrobial activity against Staphylococcus aureus and Pseudomonas aeruginosa. For qualitative and quantitaive investigations of the key aroma compounds and the compositions of the essential oils, gas chromatographic methods (GC-FID and GCMS with columns of different polarities) were used and the results correlated with that of the antimicrobial testings. The obtained data are discussed to get more insight into the influence of pure aroma compounds on antimicrobial activities of essential oils.
Modulatinn Intestinal Uptake of Atenolol Usinn Niosomes as Drun Permeation Enhancers
Authors: Alsarra lbrahim , Bosela Ahmed , Al-Mohizea Abdullah M. , Mahrous Gamal M. , Neau Steven H.
Published: May 2019

It is well established through the last decade that niosomes have potential applications as drug carriers either to improve drug permeation across membranes or targeting to specific tissues. Having a considerable ability to improve the permeability of drugs through lipoid membranes, niosomes have been utilized as carriers to enhance atenolol absorption from the gastrointestinal tract. Two methods have been adopted to prepare niosomes, the proniosome-derived method (A) and the conventional film hydration method (B). The products from the two methods were compared in terms of their morphology, vesicle size, drug encapsulation efficiency, in vitro drug release and enhancement effect on drug permeation across the intestinal membrane using an everted sac technique. Proniosome-derived niosomes were smoother and exhibited a smaller (5 μm) vesicle size compared to those prepared by conventional methods (12 μm). High encapsulation efficiencies of 98.6% and 93.4% were achieved by methods A and B, respectively. In vitro drug release has been significantly retarded from both types of niosomes. Comparing to pure drug, which dissolved completely in 15 min, only 8.9% and 9.9% of the entrapped drug was released in the same time period. The drug release kinetics showed non-Fickian (anomalous) behavior. Permeation through an everted intestinal sac showed a significant enhancement effect (more than 4 fold) for both types of niosomes compared to untrapped drug; however, the difference between the two types of niosomes was not significant
Variations of Naphthoquinone Levels in Micropropaaated Drosera Species In Vitro, under Qreenhouse and Outdoor Growth Conditions
Authors: Wawrosch Christoph , Vackar Eva , Grauwald Brigitte
Published: May 2019

The naphthoquinone levels in clones of the sundew species Drosera communis, D. madagascariensis, D. peltata and D. rotundifolia were determined under in vitro, green house, and outdoor growth conditions. D. rotundifolia revealed a lower naphthoquinone content in vitro which rose upon transfer ex vitro. D. communis and D. madagascariensis exhibited higher levels in vitro which decreased in the greenhouse and further under outdoors conditions. Decreased naphthoquinone levels were found in D. peltata when in vitro cultures were moved to the greenhouse, which increased again when the plants were cultivated outdoors. The results underline that in the cultivation of the medicinally useful carnivorous genus Drosera species-specific differences in the biosynthesis of secondary metabolites under different environmental conditions have to be taken into consideration.
Competence model for measuring career development and organisational growth in the health sector
Authors: Adeniji Anthonia , Osibanjo Omotayo , Salau Odunayo P , Falola Hezekiah O. , Igbinoba Ebegbuki , Ohunakin Folakemi , Ogueyungbo Opeyemi
Published: May 2019

The present changing trend and competitive business world have compelled many sectors to improve their service quality, productivity and performance. The health sector is a unique sector with peculiar work environment and developmental expectations from workers of different categories. Experts indicate that the Nigeria health sector budget is not impressive as it has never moved closer to World Health Organization template of 15% of the annual budget allocated to the health sector. Arising from this gross underfunding, the health sector has become weak while infrastructure and logistic supports seem to be obsolete with defective career initiative programmes. Hence, the present study assessed a competence model for measuring career development and growth of the health sector in Nigeria. The descriptive research design was adopted using stratified-random sampling technique with a mixed method (specifically, sequential explanatory method) approach for gathering data from the selected teaching hospitals. Six dimensions and 30 item statements of career development and organizational growth have been adopted from previous studies. The use of a structured questionnaire was employed and completely filled by 377 staff and management of the selected tertiary institutions. Data collected through the copies of questionnaire were analysed through measurement and structural models (SEM_PLS3); while interview data were codified and themes extracted. The results of the statistical analysis reveal that organizational growth significantly depends not only on the formulation and implementation of career development programmes but also on monitoring. The findings of this research have explicit implications for both the employees and the organizations. This study suggests that management will need to provide interventions and be more active in carefully implementing career management plans that will meet individual and organizational goals.
Was the Sun a Slow Rotator? Sodium and Potassium Constraints from the Lunar Regolith
Authors: Saxena Prabal , Killen Rosemary M. , Airapetian Vladimir , Petro Noah E. , Curran Natalie M. , Mandell Avi M.
Published: May 2019

While the Earth and Moon are generally similar in composition, a notable difference between the two is the apparent depletion in moderately volatile elements in lunar samples. This is often attributed to the formation process of the Moon, and it demonstrates the importance of these elements as evolutionary tracers. Here we show that paleo space weather may have driven the loss of a significant portion of moderate volatiles, such as sodium and potassium, from the surface of the Moon. The remaining sodium and potassium in the regolith is dependent on the primordial rotation state of the Sun. Notably, given the joint constraints shown in the observed degree of depletion of sodium and potassium in lunar samples and the evolution of activity of solar analogs over time, the Sun is highly likely to have been a slow rotator. Because the young Sun’s activity was important in affecting the evolution of planetary surfaces, atmospheres, and habitability in the early Solar System, this is an important constraint on the solar activity environment at that time. Finally, as solar activity was strongest in the first billion years of the Solar System, when the Moon was most heavily bombarded by impactors, evolution of the Sun’s activity may also be recorded in lunar crust and would be an important well-preserved and relatively accessible record of past Solar System processes.
Evaluating Local Ionization Balance in the Nightside Martian Upper Atmosphere during MAVEN Deep Dip Campaigns
Authors: Cui J. , Cao Y.-T. , Wu X.-S. , Xu S.-S. , Yelle R. V. , Stone S. , Vigren E. , Edberg N. J. T. , Shen C.-L. , He F. , Wei Y.
Published: May 2019

Combining the Mars Atmosphere and Volatile Evolution (MAVEN) measurements of atmospheric neutral and ion densities, electron temperature, and energetic electron intensity, we perform the first quantitative evaluation of local ionization balance in the nightside Martian upper atmosphere, a condition with the electron impact ionization (EI) of CO2 exactly balanced by the dissociative recombination (DR) of ambient ions. The data accumulated during two MAVEN Deep Dip (DD) campaigns are included: DD6 on the deep nightside with a periapsis solar zenith angle (SZA) of 165°, and DD3 close to the dawn terminator with a periapsis SZA of 110°. With the electron temperatures at low altitudes corrected for an instrumental effect pertaining to the MAVEN Langmuir Probe and Waves, a statistical agreement between the EI and DR rates is suggested by the data below 140 km during DD6 and below 180 km during DD3, implying that electron precipitation is responsible for the nightside Martian ionosphere under these circumstances and extra sources are not required. In contrast, a substantial enhancement in EI over DR is observed at higher altitudes during both campaigns, which we interpret as a signature of plasma escape down the tail.
Modelling Acacia saligna invasion on the Adriatic coastal landscape: An integrative approach using LTER data
Authors: Marzialetti Flavio , Bazzichetto Manuele , Giulio Silvia , Acosta Alicia T.R. , Stanisci Angela , Malavasi Marco , Carranza Maria Laura
Published: May 2019

Invasive Alien Species (IAS) pose a major threat to biodiversity and ecosystem services worldwide. Even if preventing biological invasions should be the most cost-effective way to minimise the impact of IAS on biodiversity, new efforts are necessary to identify early signs of invasion and to assess invasion risk. In this context, the implementation of invasive Species Distribution Models (iSDMs) could represent a sound instrument that merits further research. Acaciasaligna is an Australian vascular plant introduced into Europe during the last half century and is one of the most aggressive IAS in the Mediterranean basin.

In this work, we model the occurrence of A.saligna in the coastal landscapes of central Italy (Adriatic coast) while accounting for the simultaneous effect of multiple factors (propagule pressure, abiotic, biotic factors). The iSDM for A.saligna was implemented on a representative tract of the Adriatic coast in central Italy (Molise region), largely included in two Long-Term Ecological Research (LTER) sites which actively contribute to the description of the considered ecosystem status and possible future trends. By using a Generalised Linear Model (GLM) with a binomial distribution of errors based on field and cartographic geo-referenced data, we examined the statistical relationship between the occurrence of A.saligna and a comprehensive set of environmental factors. The iSDM effectively captured the role of the different variables in determining the occurrence of A.saligna in the coastal dunes. Its occurrence is primarily related to Wooded dunes with Pinuspinea and/or P.pinaster (EU Habitat 2270) and distance from the sea and, to a lesser extent, with distance from roads and rivers. This research provides a first exploratory analysis of the environmental characteristics that promote the rapid growth and development of A.saligna in Italian dune ecosystems, identifying the habitats that are mainly affected by the invasive process in coastal areas and, by doing so, contributing to filling the gap between theory and practice in conservation decision-making. Finally, the LTER network benefitted from this research, confirming its relevance in providing useful information for modelling and monitoring invasion processes.
Comparison of biological and ecological long-term trends related to northern hemisphere climate in different marine ecosystems
Authors: Kröncke Ingrid , Neumann Hermann , Dippner Joachim W. , Holbrook Sally , Lamy Thomas , Miller Robert , Padedda Bachisio Mario , Pulina Silvia , Reed Daniel C. , Reinikainen Marko , Satta Cecilia T. , Sechi Nicola , Soltwedel Thomas , Suikkanen Sanna , Lugliè Antonella
Published: May 2019

Data from five sites of the International Long Term Ecological Research (ILTER) network in the North-Eastern Pacific, Western Arctic Ocean, Northern Baltic Sea, South-Eastern North Sea and in the Western Mediterranean Sea were analyzed by dynamic factor analysis (DFA) to trace common multi-year trends in abundance and composition of phytoplankton, benthic fauna and temperate reef fish. Multiannual trends were related to climate and environmental variables to study interactions. Two common trends in biological responses were detected, with temperature and climate indices as explanatory variables in four of the five LTER sites considered. Only one trend was observed at the fifth site, the Northern Baltic Sea, where no explanatory variables were identified. Our findings revealed quasi-synchronous biological shifts in the different marine ecosystems coincident with the 2000 climatic regime shift and provided evidence on a possible further biological shift around 2010. The observed biological modifications were coupled with abrupt or continuous increase in sea water and air temperature confirming the key-role of temperature in structuring marine communities.
Seeking consensus in German forest conservation: An analysis of contemporary concepts
Authors: Demant Laura , Meyer Peter , Sennhenn-Reulen Holger , Walentowski Helge , Bergmeier Erwin
Published: May 2019

Setting operational conservation objectives is a major challenge for effective biodiversity conservation worldwide. To analyse forest conservation objectives in Germany in a transparent manner and to achieve a consistent and consensual framework, we systematically classified conservation objectives suggested in concepts by different stakeholders. We analysed 79 biodiversity and forest conservation concepts of different stakeholder groups at various scales and applied textual content analysis and Dirichlet regression to reach a high degree of transferability and applicability. Our analysis revealed a broad consensus concerning forest conservation across stakeholders and scales, albeit with slight differences in focus, but we detected a scale-related mismatch. A wide array of conservation objectives covered social, biotic and abiotic natural resources. Conservation of species, ecosystems and structural elements in forests were found to be of primary importance across stakeholders and scale levels. Shortcomings in the conservation concepts were found in addressing genetic diversity, abiotic resources and socio-cultural objectives. Our results show that problems in forest conservation may be rooted in trade-offs between aims, targeting mismatch across scale levels and insufficient implementation of objectives.