Breakthroughs in Indole and Indolizine Chemistry – New Synthetic Pathways, New Applications

Indole and indolizines (heterocyclic aromatic compounds structurally and chemically isomeric with indoles) are an important class of N-fused heterocyclic compounds due to their interesting biological and optical properties. Different strategies for generating diverse collections of small molecules with indole and indolizine moieties have been developed. They can be synthesized by means of classical and nonclassical pathways. The present study discusses the versatile nature of indole/indolizine derivatives, new green methods for their synthesis, their possible mechanism of action and also provides information about current/future prospects of the topics and different indole/indolizine derivatives in pharmaceutical/clinical trials. With the remarkable number of approved indole-containing drugs as well as the importance of the indolizine moiety, it can be easily concluded that indole and indolizine derivatives offer perspectives on how pyrrole scaffolds might be exploited in the future as bioactive molecules against a broad range of diseases

RECHERCHES SUR LE DEVELOPPEMENT DES COCKTAILS AVEC UN POTENTIEL ANTIOXYDANT ELEVE

The research aimed to study the influence of the extraction process on the content of antioxidant compounds present in four types of tea and establishing of the optimal conditions for preparation of cocktails in whose composition is combined the beneficial effect of foods rich in antioxidants and vitamins: green tea, exotic fruits, berries and honey. Content of antioxidants, protein, fiber, vitamins and minerals from unfermented tea is supplemented by high concentration of biological active compounds in fruits and honey used. A positive correlation between substances added with significant increase of antioxidant and nutritive potential has been observed. This study confirms that the synergistic action of green tea, fruits and honey allowed obtaining attractive drinks from sensorial point of view and compounds with high antioxidant potential content

Influence of spice and wine based marinades on bovine Biceps femoris muscle tenderness

Fresh beef slices were marinated by immersion in marinades based on dry red wine, lime-tree honey, salt, spices and seasoning plants as thyme (Thymus vulgaris), marjoram (Majorana hortensis), garlic (Allium sativum) and horseradish (Armoracia rusticana). Control samples were prepared without marinating treatment but packed and stored in the same conditions as marinated samples. After marination, meat pieces were packed under vacuum and stored at 4°C for 12 days. The combined effects of spices and marination on beef tenderness were evaluated by monitoring pH evolution, the protein and collagen degree of hydrolysis and tenderness. Experimental data indicated that marination weaken beef meat structure, producing improvement of functional properties of adult beef. Marinades use lead for an increase in the protein nitrogen fraction, free amino acids and hydroxyproline contents in boiled beef cuts. A significant increase in tenderness by hardness measurement was observed in the samples marinated and boiled, as compared with the control.Key words: Acidic marination, beef meat, marinating time, meat hardness, pH

The Influence of Extraction Method on the Apparent Content of Bioactive Compounds in Romanian Allium spp. Leaves

In order to characterize the composition of bioactive compounds in Allium spp., an important source of traditional foods, analysesof their physicochemical properties, total phenols, and flavonoid content were carried out using three of the most popular Romanian leafvarieties (Allium cepa var. ‘Diamant’, ‘Rubiniu’, and Allium ursinum L.). The highest levels of bioactive compounds were detected in theleaves of Allium ursinum L., 7.2730 mg QE/ kg fresh plant and 27.8884 g GAE/100 g dry basis, respectively. This study suggests potentialgood uses of the fresh leaves of Romanian Allium spp. as condiments, ingredients or preservatives in the food industry

FLUORESCENT N-HETEROCYCLES VIA ONE-POT TANDEM REACTIONS

Substituted indolizines are very attractive heterocyclic units. On developing efficient methods toward differently substituted indolizines, we were particularly interested in elaborating efficient approaches toward three-component reaction of these compounds which are very interested from the point of view fluorescent properties. The microwave-mediated three component reaction of acyl bromide, bipyridine and dipolarophyl is catalyzed by basic alumina to give corresponding bis-indolizines in excellent yields in a one –pot reaction

Pyrrolidinium octanoate carboxylate as PIL agent in the growth mechanism of lysozyme spherulites

International audienceIn this research the impact of pyrrolidinium octanoate carboxylate (PyO) on Lysozyme (Ly) spherulite forms using the method of vapour diffusion with hanging drops (HDVD) was investigated. Two different stock solutions at low alkaline pH were tested: 0.1 M NaAc (the first one) and 0.1 M TRIS hydrochloride contained 0.2 M ammonium sulfate and 25 % wt. PEG 3450 as crystallant agents (the second one). The experiments were performed at 18°C using two PyO concentrations (0.4 M and 1.6 M) in each stock solution. PyO of booth concentrations lead to the formation of Ly - SNLC (Ly single needle-like crystals), observed by optical microscopy one day after the droplets deposition, excepted the stock solution of 0.1 NaAc based on 0.4 M PyO where Ly microspheres were identified by electron scanning microscopy. The growth mechanism of the Ly spherulites of type I obtained using 0.4 M PyO in 0.1 M TRIS/crystallant agent could be summarised as follows: Ly-SNLC → Ly-like axialites → Ly spherulites of type I. The growth mechanism of the Ly spherulites of type II using 1.6 M PyO in 0.1 M TRIS/crystallant agent can be summarised as follows: Ly-SNLC → Ly-like axialites → Ly spherulites of type II

Synthesis and physico-chemical properties of a novel series of aromatic electron acceptors based on N-heterocycles

The synthesis of a novel series of N-based heterocyclic salts using a simple and efficient N-alkylation of 1,2-bis(4-pyridyl)ethane with reactive halides is reported. These compounds can be transformed into the corresponding pyridinium methylides by addition of a base. The former exhibit an unstable absorption bands at 395-410 nm. The structures of the salts were fully characterized by UV-vis, IR, NMR and MS spectroscopy and elemental analysis. The pK values of selected compounds were also determined and the acid basic equilibrium was investigated by UV-vis spectrophotometry. The thermal stability of all species was determined by thermogravimetric analysis. (C) 2012 Elsevier Ltd. All rights reserved

EVALUATION OF THE ANTIMICROBIAL EFFECTS OF NEW HETEROCYCLIC BIS-QUATERNARY AMMONIUM COMPOUNDS ON BIOFILMS

Considering the well-known mechanism of adaptable resistance of microorganisms to chemical compounds through biofilms formation and the widespread use of N-heterocyclic quaternary ammonium salts (QAC) as disinfectants, in this study we have evaluate the effect of 8 newly synthesized symmetrical and unsymmetrical diquaternary ammonium salts of 1,2-bis-(4-pyridil)-ethane on bacterial biofilms produced by three different bacterial strains. The effect of the exposure to quaternary ammonium salts on biofilm communities was investigated within biofilms obtained in a conventional testing system, on stainless steel and glass surfaces. Differential plate counts were used to characterize the developed communities and the effects of QAC exposure and the results were correlated with epifluorescence microphotographs. The data obtained revealed a significant reduction of bacterial cells in the biofilms tested with 4-7 log CFU for all the QAC