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Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Aim: The in vitro antioxidant potential of new thiazolidin-4-one derivatives of ferulic acid was evaluated according to the total antioxidant activity and ferric reducing power assays., Material and Methods: The ferric reducing power assay was based on the reduction of ferricyanide to ferrocyanide, which form in the presence of ferric chloride a Perl Prussian blue color complex. The total antioxidant activity assay was assessed using phosphomolybdenum method. The results were expressed as effective concentration (EC50) values and ascorbic acid was used as positive control. All determinations were performed in triplicate., Results: It was found that the activity of the tested compounds is influenced by the substituents on phenyl ring of the thiazolidine-4-one moiety. The most active compound was 1i, which contains 2,3-diOH as substituent on phenyl ring., Conclusions: A total of 10 new thiazolidin-4-one derivatives of ferulic acid were investigated for their in vitro antioxidant activity. The most active compound 1i (R=2,3-diOH) proved to be about 4 times more active than ferulic acid and comparable to ascorbic acid in both antioxidant assays.

Aim: To synthesize some new azetidin-2-ones of ferulic acid and to evaluate them from physicochemical and spectral point of view., Material and Methods: The synthesis was carried out in several steps: (i) obtaining the ferulic acid chloride; (ii) obtaining the ferulic acid hydrazide with hydrazine hydrate (98%); (iii) condensation of ferulic acid hydrazide with different benzaldehydes (2-hydroxy-/2-nitro-/4-chloro-/4- fluoro-/4-bromo-benzaldehyde) in order to obtain the corresponding hydrazones; (iv) cy- clization of ferulic acid hydrazones with chloroacethyl chloride in freshly distilled toluene medium and in the presence of triethylamine, resulting in the corresponding azetidin-2-ones., Results: Six new azetidin-2-ones of ferulic acid were synthesized. They were characterized in terms of their physicochemical properties and their structure was confirmed by IR and 1H-NMR spectroscopy., Conclusions: Six new azetidin-2-ones of ferulic acid were synthesized, physicochemically characterized and validated spectrally. A

Unlabelled: L-Arginine is an a-amino acid which plays important roles in different diseases or processes, such as Alzheimer disease, inflammatory process, healing and tissue regeneration and it also could be useful as an anti-atherosclerotic agent., Aim: Considering the large amount of studies on the beneficial effects of different antioxidants, this paper is focused on the evaluation of the antioxidant potential of some imine derivatives, synthesized by the authors and described in a previous article., Material and Methods: The evaluation of the antioxidant power was performed using phosphomolydenum-reducing antioxidant power (PRAP) and ferric reducing antioxidant power (FRAP) assays, tests described in the literature and which are used with some minor modifications., Results: It was found that most of the imine derivatives are more active than the L-Arginine in the PPAP and FRAP assays. The most active derivative was the compound obtained by condensation of L-arginine with 2,3-dihydroxybenzaldehyde (2k) and 2-nitrobenzaldehyde (2g)., Conclusions: Following the described protocol, some imine derivatives of L-arginine were evaluated in terms of antioxidant potential using in vitro methods. The most favorable influence was obtained by the aromatic substitution with nitro and hydroxyl, the corresponding derivatives being the most active derivatives compared to L-arginine.

Diabetes mellitus is a major health problem due to its increasing prevalence and life-threatening complications. Antidiabetic sulfonylureas represent the first-line drugs in type 2 diabetes even though the most common associated risk is pharmacologically-induced hypoglycemia. In the development of this side effect are involved several factors including the pharmacokinetic and pharmacodynamic profile of the drug, patient age and behavior, hepatic or renal dysfunctions, or other drugs associated with a high risk of interactions. If all these are controlled, the risk-benefit balance can be equal to other oral antidiabetic drugs.

Unlabelled: The ferulic acid (4-hydroxy-3-methoxy-cinnamic acid) is a phenolic compound with important antioxidant effects and which nowadays is being extensively studied for his potential indications in inflammatory and neurodegenerative diseases, hypertension, atherosclerosis, etc., Aim: The synthesis of new ferulic acid compounds with potential antioxidant activity., Material and Methods: The synthesis of the designed compounds was performed in several steps: (i) the obtaining of ferulic acid chloride by reacting of ferulic acid with thionyl chloride; (ii) the reaction between the ferulic acid chloride and hydrazine hydrate 98% to obtain the ferulic acid hydrazide; (iii) the condensation of ferrulic acid hydrazide with various benzaldehydes (2-hydroxy/3-hydroxy/4-hydroxy/2-nitro/3-nitro/4-nitro/2-methoxi/ 4-chloro/4-fluoro/4-bromo-benzaldehyde) resulting the correspond- ing hydrazones., Results: The structure of the synthesized compounds was confirmed by FT-IR spectroscopy and the evaluation of antioxidant potential was achieved by determining the total antioxidant capacity and reducing power., Conclusions: In this study new hydrazones of ferulic acid have been synthesized, physic-chemical and spectral characterized. The evaluation of antioxidant potential using in vitro methods showed the favorable influence of the structural modulation on the antioxidant effects of ferulic acid.

Sulfonamides and their different derivatives are extensively used in therapy due to their pharmacological properties. Sulfa drugs were amongst the oldest synthesized antimicrobial agents and are still widely used today to treat different microbial infections. Clinical treatment with sulfonamides has regained confidence with the use of a combination of sulfamethoxazole and trimethoprim to treat urinary tract bacterial infections. Today, they are widely used as antimicrobial agents, chiefly because of their low cost, low toxicity and excellent activity against bacterial diseases. Over the course of time, the application of sulfonamides has been extended from their use as antimicrobial agents to anticancer agents, antiglaucoma agents, inhibitors of gamma-secretase, cyclooxgenase-2 and lipoxygenase, anticonvulsivant agents, hypoglycemic agents.

Aim: To present the research results concerning enhanced antimicrobial and release properties of the chitosan derivative with sulfadiazine/hyaluronic acid polyelectrolyte complex (PEC) hydrogel., Material and Methods: The PECs have been prepared from chitosan of different molecular weight, sulfadiazine chitosan derivative and sodium hyaluronate. The complex structure was assessed by FT-IR spectroscopic method and swelling capacity was followed by weighing measurements., Results: It has been establish that chitosan derivative influenced both PEC properties and swelling capacity., Conclusions: Incorporation in PEC of the sulfadiazine chitosan is a new way to combine bacteriostatic effect of chitosan with that of sulfadiazine, to control properties, antimicrobial activity in the treatment of the wound.

Aim: This paper is a short review on the state-of-the-art of the use of polyelectrolyte complexes containing polysaccharides for wound and burn healing and treatment using the chitosan/hyaluronic acid polyelectrolyte complex (PEC) hydrogel., Results and Conclusions: PEC is suitable for wound healing because a wet treatment can be realized and both components of PEC contribute by their properties to the enhanced antimicrobial activity, promote wound healing and prevent wound damage during treatment.

Unlabelled: The International Diabetes Federation reported that 246 million adults worldwide had diabetes mellitus and the prevalence of this syndrome was expected to increase continuously., Aim: To design new compound with potential antidiabetic and antioxidant activity., Material and Methods: New benzylidene-thiazolidine derivatives (BT2a-2e) were obtained by condensation of xanthine-thiazolidine-4-one (TZ-4-one) with aromatic aldehydes. The synthesized compounds were characterized by spectral method (IR, 1H-NMR, 13C-NMR) and their antioxidant potential has been also evaluated., Results: The synthesized compounds have important antioxidant effects as compared to xanthine-thiazolidine derivatives. The most active compounds were those obtained by condensation with 4-dimethylaminobenzaldehyde (BT2c) and 4-nitro-benzaldehyde (BT2e)., Conclusions: The chemical modulations performed on the structure of TZD-4-one have a good influence on their antioxidant potential.

Objectives: Biologic therapy such as Etanercept, which is a tumor necrosis factor alpha (TNF-α) inhibitor, has been extensively used as election therapy in rheumatoid arthritis. The purpose of this case presentation was to inform about the possibility that lichen planus lesions could potentially become complicated by secondary infections in patients treated with Etanercept. Furthermore, we aimed at analyzing if the complication of the cutaneous lesion was coincidental or it was due to the immunosuppressive systemic therapy, and whether the infected lesion would respond to antibiotic therapy., Case Summary: The patient was a 59-year-old woman with rheumatoid arthritis and that have had lichen planus lesions for approximately 25 years. Only recently, she had been received immunosuppressive therapy (Etanercept and Methotrexate). Further on, the lichen planus flared up with a secondary infection determined by a Methicillin-sensitive Staphylococcus aureus. Uncommon myocardial complications were also characteristic of this case., Results: While a case report described already the appearance of lichen planus following Etanercept therapy (Battistella M et al., 2008), the possibility that the lesion could become secondary complicated following this therapy was never reported before, according to our knowledge. Additionally, we describe in this case the interplay between Etanercept therapy and hypertrophic cardiomyopathy., Conclusions: Our case is not a lichen planus induced by Etanercept, but it is aggravated and secondary infected with Methicillin-sensitive Staphylococcus during the therapy. The additional cardiac complication (hypertrophic cardiomyopathy) may represent solely an evolutive sign of rheumatoid arthritis and therefore not influenced by Etanercept.

Aim: The study was designed to present the modern therapy used for the treatment of type 2 diabetes mellitus (T2DM)., Material and Methods: Diabetes mellitus and the pharmacological and the pharmacokinetic characteristics of the incretins and of the incretin modulators are presented., Results: Diabetes mellitus is a chronic metabolic disorder, which is considered to be a major health issue all over the world. World Health Organization indicates that world-wide almost 3 million deaths per year are caused by diabetes and 1,5 million new cases are diagnosed annually, T2DM representing approximately 90-95% of the diagnosed cases. This form of diabetes mellitus is characterized by several path physiological defects including insulin resistance at peripheral target tissues, excess hepatic glucose production and progressive pancreatic beta cell dysfunction. The newest direction in the treatment of T2DM mellitus is the incretin modulators. The incretins (GLP-1--glucagon-like-peptide-1 and GIP--glucose-dependent insulin tropic peptide), are natural hormones that contribute to glucose homeostasis by acting on the pancreas, gastrointestinal tract, muscle and brain tissue. After secretion, GLP-1 and GIP are immediately metabolized by dipeptidyl peptidase IV enzyme (DPP IV), which limits their therapeutic use., Conclusions: In order to achieve optimal glycemic control, by using the therapeutic effects of incretins, research has been directed to the development of synthetic analogues of GLP-1 resistant to DPP IV enzyme inactivation and DPP IV inhibitors.

Unlabelled: Many studies show that flavonoids have a numerous biological properties, antimicrobial effects included. It is also known that rutin is able to increase the antibacterial activity of other compounds., Material and Methods: Starting from these facts, we synthesised some water soluble rutin derivatives treating rutin with 1, 3-dichloro-2-propanol, 1-bromo-3-chloro-propane, 2-dibromethane, and dibrommethane, and than with 7-amino-cephalosporanic acid. The antimicrobial activity of the new compounds was determined by disc diffusion method., Results: Molecular formula, weight, yield, melting points and solubility of the new derivatives have been determined. Elemental analysis and spectral analysis (UV and IR) confirmed the structure of new compounds. CONCLUSIONS. These derivatives are water-soluble and have a good antimicrobial activity, both on Gram-positive and Gram-negative bacteria, comparable with that of tetracycline.

Aim: The 6-aminopenicillanic acid acylation with certain acyl chlorides was performed in order to obtain antistaphylococcal penicillins with bigger crystals, easy to filtrate (shorter filtration time), much pure, and an increased output., Material and Methods: Oxacillin sodium salt was synthesized by acylating an aqueous solution of 6-aminopenicillanic acid sodium salt (NaHCO3 not in excess) with an ethylacetate solution of 5-phenyl-3-methyl-isoxazolyl-4-carboxilic acid chloride. The crystallization was performed with a 40.5% sodium 2-ethyl hexanoate izopropanolic solution. All tests (IR spectrum, iodometric titration, and microbiological dosage) were performed according to the Xth Romanian Pharmacopoeia standards., Results: The amount of synthesized oxacillin was higher and the output of 88,21%. Oxacillin had a high chemical purity (98,72%), and a very good microbiological activity (95% of the standard activity)., Conclusions: Oxacillin crystals were bigger, the filtration speed was increased, and process efficacy improved. The output of the process was also improved being higher than with classical acylation.

Unlabelled: The compounds with thiadiazine structure have numerous biological properties. They are known for antimycotic, antimicrobial, antiviral, vasodilatatory, antiarytmic, bronhodilatatory and antiagregant actions., Material and Method: In order to study the influence of the different substituents on pharmacological properties of the thiadiazine compounds new benzimidazo-pyrimidino-imidazo-thiadiazine derivatives with potential biological actions have been synthesized., Results: The optimal conditions of reaction have been established and the chemical structure of the synthesized compounds has been confirmed by elemental analysis and IR spectroscopy., Conclusions: The calculated formula according to the elemental analysis results and the spectral characteristics are in good agreement with the expected structures proposed.

Unlabelled: The behavior at degradation by soil burial of some plasticized polyvinyl chloride (PVC) based blends with a variable content of hydrolyzed collagen (HC) has been followed., Material and Method: The modifications induced in the environment by the polymer systems (pH variation, physiologic state of the plants, assimilatory pigments) were studied. Using the growth test of the terrestrial plants, we followed the development of Triticum (wheat), Helianthus annus minimus (little sunflower), Pisum sativum (pea), and Vicia X hybrida hort, during a vegetation cycle. After the harvest, for each plant, the quantities of chlorophyll and carotenoidic pigments and of trace- and macroelements were determined., Results: It was proved that, in the presence of polymer blends, the plants do not suffer morphological and physiological modifications, the products released in the culture soil being not toxic for the plants growth.

Unlabelled: In this study we tried to improve the erythromycin ethylsuccinate obtaining, having in view to separate the erythromycin ester by crystallization in water., Material and Methods: The erythromycin acylation and the erythromycin ethylsuccinate crystallization were realized, following the next steps: 1. the acylation of the erythromycin with a methylene chloride solution of monoethylsuccinyl chloride, at 25-28 degrees C for 3 hours in the presence of NaHCO3; 2. the transfer of the erythromycin ethylsuccinate from methylene chloride solution in acetone solution by distillation of mixture methylene chloride: acetone 1:1 at 25-28 degrees C; 3. erythromycin ethylsuccinate separation by crystallization in water at pH = 8-8.5 and 5 degrees C for 90 minutes. The quality control for the erythromycin ester was performed according to the Xth edition of Romanian Pharmacopoeia standards using national standard for erythromycin ethylsuccinate and national standard for erythromycin with an activity of 1: 937 U and 2.02% humidity. The Micrococcus luteus ATCC 9341 was used as a test microorganism and a thin layer cromatography was performed for qualitative control., Results: 13.1 g of erythromycin ethylsuccinate were obtained with an output of the process of 82.02%. Using water for the separation of erythromycin ethylsuccinate the output of the process is greater (82.02%) than in case of using petroleum ether (74.14%) or hexane (80.25%). The thin layer cromatography revealed an Rf = 0.56 and the microbiological activity of the erythromycin ethylsuccinate was 98.7% compared with the standard., Conclusions: Using water instead of hexane or petroleum ether is gainful for the separation of erythromycin ethylsuccinate from the reaction medium. The obtained erythromycin ethylsuccinate corresponds to the Xth edition of Romanian Pharmacopoeia standards. So, the raw materials consumption is decreased, the costs are cut down, the obtained product purity is high and the output of the process is greater.

Unlabelled: Isoniazid is one of the most used antituberculosis drugs, but its toxicity is high. In this study, four derivatives of rutin and isoniazid were prepared and their antibacterial and antimycotic activities were investigated., Method: Synthesis of these compounds started through reaction of rutin with fresh prepared sodium methoxide, subsequently treating with 1, 3-dichloro-2-propanol, 1-brom-3-chloropropane, 1, 2-dibrom-ethane or dibrommethane and finally, stirring with isoniazid, to afford crystalline, yellow, water soluble powders., Results: The four compounds were marginally active against Staphylococcus aureus and Staphylococcus saprophyticus and were inactive against Escherichia coli., Conclusion: We synthesised four new derivatives of rutin and isoniazid; melting points, solubility, yields characterised these compounds, and their structure was confirmed by C, H, N elemental analysis and UV spectra. The compounds showed a modest antibacterial activity. We think that the toxicity of the new derivatives will be lower that of isoniazid toxicity. The next steps in our research will be the toxicological study and antituberculosis assay.

In order to obtain new compounds with potential antimicrobial activity some new (sulfon-amidophenyl)-amide derivatives of N-(m-nitrobenzoil)-D,L-methionine have been synthesized. The compounds have been obtained by decyclization reaction of 2-(m-nitrophenyl)-4-(beta-P-methylthioethyl)- delta2-5-oxazolinone with various sulfonamides. The chemical structure of the new sulfonamides was confirmed by elemental analysis data and IR and 1NMR spectral measurements. The compounds were also investigated for their antimicrobial activity using Staphylococcus aureus, Escherichia coli, Listeria monocytogenes and Proteus vulgaris strains.

Fibrates are drugs with efficacy in reducing blood cholesterol levels and especially, triglyceride plasma levels. Unfortunately, fibrates have a poor water-solubility and showed some adverse reactions at long treatment. The objective of this study was to obtain some new clofibric acid derivatives with rutin; some of these compounds contain a guanidine moiety, known as effective at cardiovascular level. All the compounds are soluble in water.

In order to obtain new compounds with potential antibacterial activity some new (sulfonamidophenyl)-amide derivatives of N-(m-nitrobenzoil)-D,L-asparagine have been synthesized. The compounds have been obtained by decyclization reaction of 2-(m-nitrophenyl)-4-(beta-amidomethyl)-delta2-oxazolinone with various sulfonamides. A toxicity study with determination of DL50 value has also been realized.

The effects of some new methylxanthine compounds, derivatives of theophylline, theobromine and caffeine with various radicals in 8 position on blood pressure have been studied. Derivatives of theophylline (1,3-dimethyl-xanthine) with various radicals in 8 position have reduced the blood pressure. In the same experimental conditions the theobromine (3,7-dimethyl-xanthine) derivatives haven't modified the blood pressure while the caffeine (1,3,7-trimethyl-xanthine) derivatives have increased the blood pressure values.

We have synthesized new xanthine compounds, derivatives of theophylline with various radicals in 7 position. The compounds have been characterized by molecular formula, weight, yield and melting point. The synthesized xanthine derivatives have been purified by repeated crystallizations from various organic solvents. Their chemical structure was confirmed by IR spectroscopy.

We studied the potentially anti-inflammatory action of some new xanthine compounds, theophylline derivatives with 7-[2-hydroxy-3-(4-acetamido)-phenoxy-propyl]-8-R-1,3-dimethyl-xanthine and 8-R-1,3-bis-(1,3-dimethyl-xanthin-7yl)-2-hydroxy-propane structure substituted in 7 and 8 position. Almost all studied compounds reduced the inflammatory edema, the effect being comparable or highest theophylline. The antiinflammatory effect of theophylline intensified with the introduction in 7 position the theophylinyl radical and in 8 position the bromo, nitro, pirolidinyl, piperidinyl, morfolinyl, imidazolyl, 3,5-dimethyl-pirazolyl, 3-methyl-5-oxo-pirazolyl radicals.