Synthesis and anti-proliferative activity studies of 2-(2-(trifluoromethyl)-6-(substituted)imidazo[1,2-b]pyridazin-3-yl)-N-(substituted)acetamide derivatives

A series of novel imidazo[1,2-b]pyridazin-3-yl acetamide derivatives (9a-9j) were synthesized from a 3,6-dichloropyridazine. We have developed a simple strategy for the synthesis of functionally diverse imidazole, and pyridiazine derivatives were reported via a series of steps. The work involves bicyclic imidazo-pyridazine ring formation, halogenation, cynation, hydrolysis, peptide coupling, and Buchwald reaction. The structure of the synthesized compounds was confirmed by IR, ¹H NMR, ¹³C NMR,¹⁹F NMR, mass spectra, and elemental analysis, and purity is checked by HPLC. All synthesized compounds were screened for anticancer activity against A-549 and Du-145 cancer cell lines by MTT assay. The preliminary bioassay suggests that most of the compounds show anti-proliferation with different degrees; doxorubicin was used as positive control. The synthesized compound shows IC₅₀ values in the range of 1.74μM to 16.17μM in both cell lines. The compounds 9e , 9g , and 9h were active compared with doxorubicin in both the cell lines. The compounds having cyclopentyl ring are active compared with higher and lower carbon analogues.     

Preparation and characterization of submicron hybrid magnetic latex particles

Micrometer magnetic hybrid particles are of great interest in biomedical field, and various morphologies have been prepared via encapsulation processes. Regarding submicron, only few processes have been investigated and the most recent one leading to highly magnetic submicron magnetic hybrid particles is based on oil in water magnetic emulsion (MES) transformation. The encapsulation of magnetic iron oxide nanoparticles forming oil in water MES was investigated using different styrene/cross‐linker divinylbenzene volume ratio in the presence of potassium persulfate initiator. The encapsulation performed in this work is basically conducted by using well‐defined oil in water MES as a seed in radical emulsion polymerization. The chemical composition, morphology, iron oxide content, magnetic properties, electrokinetic properties, particle size, and size distribution of the prepared magnetic hybrid particles were examined using various techniques. The desired perfect magnetic core and polymer shell morphology were successfully obtained, and the final magnetic hybrid particles are superparamagnetic in nature and exhibit high iron oxide content (64 wt %). Copyright © 2015 John Wiley & Sons, Ltd.     

A novel iridoid glycoside from the aerial parts of the Tunisian Prasium majus

Repeated fractionation of the acetylated methanol extract of Prasium majus afforded acetylated derivatives of a new iridoid glycoside hamighriprasin (1), myoporoside (2), beta-D-glycopyranose (3) and saccharose (4). The structures of 1 and 2 were established by interpretation of 1D and 2D NMR data of their corresponding acetylated derivatives and by comparison with the literature.     

Lacitemzine, a novel sesquiterpene acid from the Tunisian plant Pulicaria laciniata (Coss. et Kral.) Thell.

The flowers of Pulicaria laciniata (Coss. et Kral.) Thell. (Asteraceae) afforded a new sesquiterpene acid 1, named lacitemzine together with the three known compounds, 4-hydroxy-3-methoxypyridine 2, β-sitosterol-3-O-β-d-glucoside 3 and 1,3,5-trimethoxybenzene 4. The structure of compound 1, 2-(2,6-dimethyl-3,4,5,6,7,8,9,10-octahydro-5,8-oxaazulen-9-yl)acrylic acid, contains a guaiane skeleton and was elucidated by spectroscopic procedures including 2D-NMR and X-ray diffraction.     

Efficient Synthesis of Chiral 1,1′‐Sulfonyl Bisaziridines

An efficient three‐step synthesis of chiral 1,1′‐(sulfonyl)bisaziridines is described. Preparation of these compounds was carried out easily starting from N,N′‐sulfonyl bis‐(α‐L‐aminoester) to afford the title compounds in very good yields. These 1,1′‐(sulfonyl)bisaziridines can constitute interesting synthetic building blocks.     

Antimicrobial and antioxidant activities of the methanolic extracts of three Salvia species from Tunisia

This study examines the in vitro antimicrobial and antioxidant activities of the methanolic extracts of three Salvia species from Tunisia: Salvia aegyptiaca L., S. argentea L. and S. verbenaca Ssp. clandestina L. Pugsley. The extracts inhibited the growth of dermatophytes and of bacteria responsible for unpleasant odours to varying degrees; the pathogenic yeasts Candida albicans and Cryptococcus neoformans, the filamentous fungi Aspergillus fumigatus and selected dog otitis bacteria were all resistant to each of the extracts. The extracts were screened for their antioxidant activities using 2,2-diphenyl-1-picrylhydrazyl free radical scavenging and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) test systems, and gave positive results in both tests. The extracts of S. aegyptiaca were the most active in both tests, followed by those of S. verbenaca, then S. argentea. These results confirm the antimicrobial and antioxidant activities of the genus Salvia and underline the potential of these plants either as natural preservatives or in pharmaceutical applications.     

A convenient synthesis of a novel fused tetracyclic heterocoumarin

New tetracyclic 6H‐[1]benzopyrano[3,4‐e]pyrazolo[1,5‐a]pyrimidin‐6‐ones ( 4a‐e ) have been synthesized through the condensation under acidic conditions of [1]benzopyrano[4,3‐c][1,5]‐benzodiazepin‐7(8H)‐one ( 1 ) and a series of 3,4‐disubsituted 5‐amino‐1H‐pyrazoles 3a‐e .     

Poly(p‐phenylenediamine)‐coated magnetic particles: Preparation and electrochemical properties

Magnetic particles are of great interest in various biomedical applications, such as, sample preparation, in vitro biomedical diagnosis, and therapy. For biosensing applications, the used functional magnetic particles should answer numerous criteria such as; submicron size in order to avoid rapid sedimentation, high magnetic content for fast separations under applied magnetic field, and finally, good colloidal stability. Therefore, the aim of this work was to prepare submicron magnetic core and conducting polymer shell particles. The polymer shell was induced using p‐phenylenediamine as key monomer. The obtained core–shell particles were characterized in terms of particle size, size distribution, magnetization properties, Fourier transform infrared (FTIR) analysis, surface morphology, chemical composition, cyclic voltammetry, and impedance spectroscopy. The best experimental condition was found using 40 mg of povidone (PVP—stabilizing agent) and 0.16 mmol of p‐phenylenediamine. Using such initial composition, the core‐shell magnetic nanoparticles shown a narrowed size distribution around 290 nm and high magnetic content (above 50%). The obtained amino containing submicron highly magnetic particles were found to be a conducting material and superparamagnetic in nature. These promising conducting magnetic particles can be used for both transport and lab‐on‐a‐chip detection.     

Biosensor for the oxidative stress biomarker glutathione based on SAM of cobalt phthalocyanine on a thioctic acid modified gold electrode

Journal of Solid State Electrochemistry - Self-assembled monolayer (SAM) of cobalt teraaminophthalocyanine (CoTAPc) was developed on thioctic acid (TA) dithiol modified gold electrode and...