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The Journal of Croatian Pharmaceutical Society

Acta Pharmaceutica

5-Acyl-8-hydroxyquinoline-2-(3'-substituted-4'-aryl-2,3-dihydrothiazol-2'-ylidene)hydrazones, <bold>5a-e</bold> to <bold>10a-c</bold>, were prepared by the reaction of appropriate 5-acyl-8-hydroxyquinoline-4-substituted thiosemicarbazones <bold>3a-e</bold> and phenacyl bromides <bold>4a-e.</bold> Structures of the new compounds were verified on the basis of spectral and elemental analyses. Twenty-eight new compounds were tested for their possible antimicrobial activities. Most of the tested compounds showed weak to moderate antibacterial activity against most of the bacterial strains used in comparison with gatifloxacin as a reference drug. The test compounds showed weak to moderate antifungal activity against tested fungi in comparison with ketoconazole as a reference drug. On the other hand, the newly synthesized compounds were tested for their anti-inflammatory effects and most of them showed good to excellent anti-inflammatory activity compared to indomethacin. Moreover, ulcerogenicity and the median lethal dose (<italic>LD</italic>50) of the most active anti-inflammatory compounds <bold>6b</bold> and <bold>9e</bold> were determined in mice; they were non-toxic at doses up to 400 mg kg-1 after <italic>i.p.</italic> administration.

Synthesis and biological activities of new substituted thiazoline-quinoline derivatives

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71526, Egypt

Keywords

<article-title>Synthesis and biological activities of new substituted thiazoline-quinoline derivatives</article-title>

β-Human chorionic gonadotropin (β-hCG) was successively labeled with [67Ga]-gallium chloride after conjugation with freshly prepared diethylenetriaminepentaacetic acid dianhydride (ccDTPA). After solid phase purification of the radiolabeled hormone, high performance liquid chromatography showed radiochemical purity higher than 95 % under optimized conditions (specific activity = 22-23 TBq mM-1, labeling efficiency 80 %). Preliminary <italic>in vivo</italic> studies (ID g-1, %) in male wild-type rats showed marked gonadal uptake of the tracer after 240 minutes in agreement with the biodistribution studies and reported β-hCG receptors. Target to blood ratios were 5.1 and 15.2 after 3 and 24 hours, respectively, while target to muscle ratios were 35 and 40 after 3 and 24 hours, respectively.

Development of a radiolabeled β-human chorionic gonadotropin

Nuclear Medicine Research Group Agricultural Medical and Industrial, Research School (AMIRS-NSTRI), Karaj, Iran

Islamic Azad University, Science and Research, Branch P. O. Box 14155-775, Tehran, Iran

Islamic Azad University, Young Researcher Club Takestan, Branch, Iran

<article-title>Development of a radiolabeled β-human chorionic gonadotropin</article-title>

{"article-title":"Development of a radiolabeled β-human chorionic gonadotropin"}

Various 6-aralkyl-9-substituted-6<italic>H</italic>-indolo[2,3-<italic>b</italic>]quinoxalines were synthesized by
reaction of 1,5-disubstituted 2,3-dioxo-2,3-dihydroindole with orthophenylene diamine.
Appreciable anticancer activity of compounds <bold>5b</bold>, <bold>5d</bold>, <bold>5g</bold> and <bold>5l</bold> at various cell lines among 59 human tumor cell panels was
observed. All the synthesized compounds were evaluated for cytostatic

activity against human Molt 4/C8 and CEM T-lymphocytes as well as for murine L1210 leukemia cells. Compound <bold>5h</bold> exhibited an <italic>IC</italic>50
of 71 µmol mL-1

against Molt 4/C8 and 117 µmol mL-1 against CEM compared to melphalan
3.2 µmol mL-1

and 2.5 µmol mL-1,
respectively. The <italic>IC</italic>50 for
compound <bold>7i</bold> against L1210 was 7.2 µmol mL-1

compared to melphalan 2.1 µmol
mL-1.

Synthesis, anticancer and cytostatic activity of some 6-indolo[2,3-]quinoxalines

Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560010, India

Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium

<article-title>Synthesis, anticancer and cytostatic activity of some 6<italic>H</italic>-indolo[2,3-<italic>b</italic>]quinoxalines</article-title>

Hexane, chloroform, ethyl acetate and ethanolic extracts of the aerial parts of <italic>Centaurea austro-anatolica</italic> Hub.-Mor. (<italic>Asteraceae</italic>) were evaluated against microorganisms, including multiresistant bacteria, using a paper disc diffusion method. The chloroform extract exhibited significant antibacterial activity toward all bacteria tested. The chemical composition of the chloroform extract was determined by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The major compounds of the extract were caryophyllene oxide (21.32 %), spathulenol (10.86 %), <italic>n</italic>-tricosanol (9.58 %) and geranyl isovalerate (8.71 %).

Chemical composition of endemic  and studies of its antimicrobial activity against multi-resistant bacteria

Department of Biology, Faculty of Arts and Sciences, Mugla University, 48121 Kotekli-Mugla, Turkey

Medical Laboratory Program Vocational School of Health Services, Mugla University, 48700 Marmaris-Mugla, Turkey

Department of Nursing Health College, Usak University, 64100 Usak, Turkey

Department of Chemistry Faculty of Arts and Sciences, Mugla University, 48121 Kotekli-Mugla, Turkey

<article-title>Chemical composition of endemic <italic>Centaurea austro-anatolica</italic> and studies of its antimicrobial activity against multi-resistant bacteria</article-title>

A new approach to the spectrophotometric determination of metronidazole (MZ) and tinidazole (TZ) has been developed. The procedure involves coupling of diazotized nitroimidazoles with <italic>p</italic>-dimethylaminobenzaldehyde (DMAB) to form a greenish-yellow solution. Optimal temperature and time were 0 °C (iced) and 3 minutes for diazotization and 30 °C and 2 minutes for coupling for both MZ and TZ. Coloured adducts of MZ and TZ showed shoulders at 406 nm and 404 nm, respectively, which were selected as analytical wavelengths. The reaction with <italic>p</italic>-DMAB occurred in a 1:1 mole ratio. Beer's law was obeyed within the 4.8-76.8 μg mL-1 concentration range with low limits of detection. The azo adducts were stable for over a week. Molar absorptivities were 1.10 × 103 (MZ) and 1.30 × 103 L mol-1 cm-1 (TZ). Overall recoveries of MZ and TZ from quality control samples were 103.2 ± 1.3 and 101.9 ± 1.3% over three days. There was no interference from commonly utilized tablet excipients. No significant difference was obtained between the results of the new method and the BP titrimetric procedures. The azo approach using the <italic>p</italic>-dimethylaminobenzaldehyde procedure described in this paper is simple, fast, accurate and precise. It is the first application of DMAB as a coupling component in the diazo coupling reaction.

A new approach to the spectrophotometric determination of metronidazole and tinidazole using -dimethylaminobenzaldehyde

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria

<article-title>A new approach to the spectrophotometric determination of metronidazole and tinidazole using <italic>p</italic>-dimethylaminobenzaldehyde</article-title>

Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (<italic>DE</italic>30 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad Maharashtra-415124, India

<article-title>Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407</article-title>

The objective of the present work was to develop a suitable transdermal drug delivery system for nitrendipine. Polymeric films of nitrendipine were prepared by the film casting technique (glass ring) on mercury substrate. They were evaluated for physicochemical parameters, <italic>in vitro</italic> release and <italic>ex vivo</italic> permeation (heat separated human epidermis). Release of the drug from the films followed anomalous transport (0.5 &lt; <italic>n</italic> &lt; 1).

Formulation and evaluation of monolithic matrix polymer films for transdermal delivery of nitrendipine

ITS-Paramedical (Pharmacy) College, Ghaziabad, India

D. J. College of Pharmacy, Ghaziabad, India

Deparment of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi, India

<article-title>Formulation and evaluation of monolithic matrix polymer films for transdermal delivery of nitrendipine</article-title>

A simple and convenient route is described for the synthesis of novel hetero 1,3-diaryl-2-propen-1-ones (chalcones) by using recyclable PEG-400 as an alternative reaction solvent. The reaction is clean with excellent yield, shorter reaction time and reduces the use of volatile organic compounds (VOCs). All the synthesized compounds were evaluated for their antimicrobial activities against several pathogenic representatives.

An improved procedure for synthesis of some new 1,3-diaryl-2-propen-1-ones using PEG-400 as a recyclable solvent and their antimicrobial evaluation

Organic Research Laboratory Department of Chemistry, Yeshwant Mahavidyalaya, Nanded-431602 (M.S) India

<article-title>An improved procedure for synthesis of some new 1,3-diaryl-2-propen-1-ones using PEG-400 as a recyclable solvent and their antimicrobial evaluation</article-title>

The potential for nasal delivery of losartan, a drug with poor oral bioavailability, was investigated using Calu-3 cells. Epithelial permeation of the drug with or without dimethyl-β-cyclodextrin (DM-β-CD) and glycocholate was investigated. Possible transport mechanism of the compound and epithelial mucosal tolerance were screened. Reversibility of epithelial membrane perturbation was also investigated by measuring transepithelial electrical resistance (TEER) recovery over a 24-h period following drug formulation exposure. The permeability coefficient of losartan was 1.3 ± 0.5 × 10-6 cm s-1. This flux was not significantly different from that of formulations containing DM-β-CD (0.5 and 1.0%) or glycocholate (0.5%). However, the formulation with 1.0% glycocholate significantly increased losartan permeation 7-fold. Losartan flux across the cells was concentration-dependent. Serosal to mucosal permeation was significantly higher than mucosal to serosal permeation. Concentration-dependency, as well as polarity in transport indicated that the flux of the compound across Calu-3 cells was not limited to passive diffusion. Cells exposed to DM-&amp;bT-CD (0.5 and 1.0%) and glycocholate (0.5%) caused no significant change in TEER and mitochondrial dehydrogenase activity (MDH). The results of the study showed that losartan may be a suitable drug candidate for nasal delivery.

Permeation of losartan across human respiratory epithelium: An  study with Calu-3 cells

Biopharmaceutics and Drug Delivery Laboratory, College of Pharmacy, Faculty of Health Professions, Dalhousie University, Halifax NS, Canada B3H 3J5

Pharmacokinetics and Metabolism Laboratory, College of Pharmacy Faculty of Health Professions, Dalhousie University, Halifax NS, Canada B3H 3J5

<article-title>Permeation of losartan across human respiratory epithelium: An <italic>in vitro</italic> study with Calu-3 cells</article-title>

Various <italic>N</italic>-(5-chloro-6-substituted-benzothiazol-2-yl)-<italic>N'</italic>-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (<bold>5a-t</bold>) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100% indicative of the promising nature of the compounds against seizure spread. Compounds <bold>5b</bold> and <bold>5c</bold> showed complete protection against MES induced seizures.

Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India

Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India

Department of Biochemistry, Faculty of Medicine, 7th October University, Misurata, Libya

<article-title>Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity</article-title>

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Editor-in-Chief Svjetlana Luterotti, Zagreb, Croatia Managing Editor Maja Jakševac Mikša, Croatian Pharmaceutical Society, Zagreb, Croatia Editorial Board Karmela Barišić (Zagreb) Jelena Filipović-Grčić (Zagreb) Mojca Kerec Kos (Ljubljana) Danijel Kikelj (Ljubljana) Jasmina Lovrić (Zagreb) Svjetlana Luterotti (Zagreb) Željan Maleš (Zagreb) Janja Marc (Ljubljana) Željka Vanić Branka Zorc (Zagreb) Alenka Zvonar Pobirk (Ljubljana) Language Editor Maja Beus, Croatia Technical Editor Branka Zorc, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia Contact Professor Svjetlana Luterotti, PhD Editor-in-Chief Croatian Pharmaceutical Society, Masarykova 2, 10 000Zagreb, Croatia phone: +385 1 63 94 433 fax: +385 1 48 56 201 e-mail: <A href="mailto:svjetlana.luterotti@gmail.com">svjetlana.luterotti@gmail.com</A>; <A href="mailto:svjetlana.luterotti@pharma.hr">svjetlana.luterotti@pharma.hr</A> Professor Branka Zorc, PhD Technical Editor Faculty of Pharmacy and Biochemistry University of Zagreb, HR-10000 Zagreb, Ante Kovačića 1 phone: +385 1 37 55 318 e-mail: <A href="mailto:bzorc@pharma.hr">bzorc@pharma.hr</A> Section Editors Karmela Barisic Mojca Kerec Kos Janja Marc Željka Vanić Maja Jakševac-Mikša, PhD Manging Editor Croatian Pharmaceutical Society HR-10000 Zagreb, Masarykova 2 phone: +385 1 48 72 849 fax: +385 1 48 72 853 e-mail: <A href="mailto:maja.jaksevac-miksa@zg.t-com.hr">maja.jaksevac-miksa@zg.t-com.hr</A> Publisher De Gruyter Poland Bogumiła Zuga 32A Str. 01-811 Warsaw, Poland T: +48 22 701 50 15

<DIV align=justify> Please submit your manuscripts to Acta Pharmaceutica via email to: <A href="mailto:svjetlana.luterotti@gmail.com">svjetlana.luterotti@gmail.com</A> or <A href="mailto:svjetlana.luterotti@pharma.hr">svjetlana.luterotti@pharma.hr</A> Open Access Statement The journal is an Open Access journal that allows a free unlimited access to all its contents without any restrictions upon publication to all users. <A href="https://content.sciendo.com/supplemental/journals/acph/acph-overview.xml/Open_Access_License.doc">Open Access License</A> </DIV>

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Volume 59 (2009): Issue 4 (December 2009)

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