Complexes of Ibuprofen Thiazolidin-4-One Derivatives with β-Cyclodextrin: Characterization and In Vivo Release Profile and Biological Evaluation.

Generally, NSAIDs are weakly soluble in water and contain both hydrophilic and hydrophobic groups. One of the most widely used NSAIDs is ibuprofen, which has a poor solubility and high permeability profile. By creating dynamic, non-covalent, water-soluble inclusion complexes, cyclodextrins (CDs) can increase the dissolution rate of low aqueous solubility drugs, operating as a drug delivery vehicle, additionally contributing significantly to the chemical stability of pharmaceuticals and to reducing drug-related irritability.

Recent Biomedical Approaches for Chitosan Based Materials as Drug Delivery Nanocarriers.

In recent decades, drug delivery systems (DDSs) based on nanotechnology have been attracting substantial interest in the pharmaceutical field, especially those developed based on natural polymers such as chitosan, cellulose, starch, collagen, gelatin, alginate and elastin. Nanomaterials based on chitosan (CS) or chitosan derivatives are broadly investigated as promising nanocarriers due to their biodegradability, good biocompatibility, non-toxicity, low immunogenicity, great versatility and beneficial biological effects. CS, either alone or as composites, are suitable substrates in the fabrication of different types of products like hydrogels, membranes, beads, porous foams, nanoparticles, in-situ gel, microparticles, sponges and nanofibers/scaffolds.

Formulation and Characterization of New Polymeric Systems Based on Chitosan and Xanthine Derivatives with Thiazolidin-4-One Scaffold.

In the past many research studies have focused on the thiazolidine-4-one scaffold, due to the important biological effects associated with its heterocycle. This scaffold is present in the structure of many synthetic compounds, which showed significant biological effects such as antimicrobial, antifungal, antioxidant, anti-inflammatory, analgesic, antidiabetic effects. It was also identified in natural compounds, such as actithiazic acid, isolated from strains.

Synthesis of [1,3,4]Thiadiazolo[3',2':1,2]imidazo[4,5-c]quinolines including Pictet-Spengler Reaction and Exploration of Their C-2 Reactivity through SAr.

This work reports the design of [1,3,4]thiadiazolo[3',2':1,2]imidazo[4,5-c]quinolines using a Pictet-Spengler reaction. The scope of the reaction was achieved from 6-(2-aminophenyl)imidazo[2,1-b][1,3,4]thiadiazole derivatives and available aldehydes. A wide range of aldehydes were employed to examine the scope of the cyclization.

Synthesis and biological evaluation of the new 1,3-dimethylxanthine derivatives with thiazolidine-4-one scaffold.

Background: The xanthine structure has proved to be an important scaffold in the process of developing a wide variety of biologically active molecules such as bronchodilator, hypoglycemiant, anticancer and anti-inflammatory agents. It is known that hyperglycemia generates reactive oxygen species which are involved in the progression of diabetes mellitus and its complications. Therefore, the development of new compounds with antioxidant activity could be an important therapeutic strategy against this metabolic syndrome.

Synthesis and biological evaluation of new 1,3-thiazolidine-4-one derivatives of nitro-l-arginine methyl ester.

Background: l-Arginine is a semi-essential aminoacid with important role in regulation of physiological processes in humans. It serves as precursor for the synthesis of proteins and is also substrate for different enzymes such as nitric oxide synthase. This amino-acid act as free radical scavenger, inhibits the activity of pro-oxidant enzymes and thus acts as an antioxidant and has also bactericidal effect against a broad spectrum of bacteria.

ISOLATION, CHARACTERIZATION AND ANTIOXIDANT ACTIVITY OF THE CRUDE POLYSACCHARIDE FROM PHYLLOPHORA PSEUDOCERANOIDES.

Unlabelled: The red seaweed Phyllophora pseudoceranoides (Gmelin) New. et Tayl, commonly found in the Romanian Black Sea coastal waters, has not been studied regarding its chemical composition and biological activities.

Aims: The aim of the present study was to isolate, characterize and assess the in vitro antioxidant activity of the crude polysaccharide from P.

New hydrazones of ferulic acid: synthesis, characterization and biological activity.

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.

Vernonia kotschyana roots: therapeutic potential via antioxidant activity.

The roots of Vernonia kotschyana Sch. Bip. ex Walp.

Design, synthesis and the biological evaluation of new 1,3-thiazolidine-4-ones based on the 4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one scaffold.

New thiazolidine-4-one derivatives based on the 4-aminophenazone (4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one) scaffold have been synthesized as potential anti-inflammatory drugs. The pyrazoline derivatives are known especially for their antipyretic, analgesic and anti-inflammatory effects, but recently there were synthesized new compounds with important antioxidant, antiproliferative, anticancer and antidiabetic activities. The beneficial effects of these compounds are explained by nonselective inhibition of cyclooxygenase izoenzymes, but also by their potential scavenging ability for reactive oxygen and nitrogen species.

Synthesis and biological evaluation of new 1,3-thiazolidine-4-one derivatives of 2-(4-isobutylphenyl)propionic acid.

New thiazolidine-4-one derivatives of 2-(4-isobutylphenyl)propionic acid (ibuprofen) have been synthesized as potential anti-inflammatory drugs. The structure of the new compounds was proved using spectral methods (FR-IR, 1H-NMR, 13C-NMR, MS). The in vitro antioxidant potential of the synthesized compounds was evaluated according to the total antioxidant activity, the DPPH and ABTS radical scavenging assays.

Development and optimization of the synthesis of new thiazolidin-4-one derivatives of ibuprofen.

Unlabelled: Ibuprofen, an important nonsteroidal anti-inflammatory agent, is one of the most prescribed drugs for the treatment of pain and inflammation from various rheumatic diseases, but some side effects can occur on long-term use.

Aim: The method for synthesis optimization of new derivatives of Ibuprofen with thiazolidin-4-one moiety, with improved pharmacological and toxicological profile.

Material And Methods: To optimize the derivatization method of free carboxyl group of Ibuprofen (2-(4-isobutylphenyl)propionic acid) the reaction conditions were varied (reagent ratio, catalyst, reaction medium).

Synthesis, characterization and antioxidant activity of some new thiazolidin-4-one derivatives.

Aim: To design new thiazolidin-4-ones derivatives and to evaluate their potential antioxidant effects using in vitro methods.

Material And Methods: New ethyl esters of the 2-(R-phenyl)-4-oxo-thiazolidin-3-yl propionic acid were synthesized using "one step reaction" between different aromatic aldehydes, thioglycolic acid and beta-alanine ethyl ester hydrochloride. The antioxidant potential of the synthesized compounds was evaluated using the DPPH radical scavenging assay and phosphomolybdenum method.

New hydrazones with pyrazolone structure: synthesis, characterization and biological evaluation.

Aim: To design new hydrazones with pyrazolone structure with improved biological properties.

Material And Methods: New hydrazones of antipyrine have been prepared by reaction of 4-aminophenazone (4-aminoantipyrine) with chloracetylchoride and hydrazine hydrate and then condensation with various aromatic aldehydes.

Results: The synthesized compounds were screened for their antibacterial activity against Gram positive (Staphylococcus aureus ATCC 25923, Sarcinalutea ATCC 9341, Bacillus cereus ATCC 14579, Bacillus subtilis) and Gram negative bacterial strains (Escherichia coli ATCC 25922) and pathogenic yeasts (Candida albicans ATCC 10231, Candida sake, Candidaglabrata).

New derivatives of aryl-propionic acid. Synthesis and biological evaluation.

Aim: To design new derivatives of aryl-propionic acid with potential antibacterial and antioxidant activity.

Material And Methods: New hydrazone of ibuprofen (2-(4-isobutylphenyl)propionic acid) have been synthesized by reaction of ethyl ester of ibuprofen with hydrazine hydrate and then condensation of corresponding hydrazide with various aromatic aldehydes.

Results: The synthesized compounds were screened for their antibacterial activity against Gram positive (Staphylococcus aureus ATCC 25923, Sarcinalutea ATCC 9341, Bacillus cereus ATCC 14579, Bacillus subtilis) and Gram negative bacterial strains (Escherichia coli ATCC 25922).