Using of some novel derivatives of thiourea for Synthesis of pharmaceutical compounds of 5-Arylidine-2-imino-4-thiazolidinones and their medicinal properties study as anti-inflammatory agents

Thiazolidinone belongs to important groups of heterocyclic compounds. Recently this compounds displays activities such as antioxidants, anti-inflammatory, anti-virus and tuberculostatic. In this project we reported an effective reaction to synthesis of novel thiazolidinone-4-one in the presence of deep Eutectic Solvent as catalyst by Aldol condensation, derivatives of thiourea asymmetric and aldehydes.The primary deivatives phenyl thiourea were obtained by the reaction of derivatives Aniline with Ammonium thiocyanate and HCl in refluxing free solvent and Next reaction between deivatives phenyl thiourea and chloro acetyl chloride in refluxing ethanol. Subsequent synthesis of 5-Arylidene-2-imino-4-thiazolidinones was performed by condensation of amino thiazolidinone with aldehydes in the presence of catalysts Deep Eutectic Solvent. This method have several advantage such as synthesis free solvent, short duration of action, the use of catalysts deep eutectic solvent, being environmentally friendly and simple procedure.The structure of synthesized compounds (3f-h) characterized by infra-red spectroscopy (FTIR), 1H Nuclear magnetic resonances, and 13C Nuclear magnetic resonances

Using of Naproxen drug for novel synthesis of 4-thiazolidinone derivatives and application of these drugs as no steroidal anti-inflammatory drug (NSAIDs) and as anti-epileptic agent

Non-steroidal anti-inflammatory drugs (NSAIDs) are now one of the most frequent drugs used in treatment of pain, inflammation and fever. In this study the aim is the synthesis of derivatives of 4-Tiazolidinon from naproxen with the possible anti-pain effects, and the main purpose of providing these derivatives is to achieve a compound with more anti-pain power and less side effects in comparison with applied drugs in clinics. Synthesis of these derivatives is done on chloride in presence of a group of new liquids like recyclable ionic liquids choline chloride, which the main advantages of these ionic liquids are the cheapness, availability, being non-toxic, and easy recyclability. This reaction was done in four stages. All the structures were verified by using data of spectrum testing, 1H-NMR, FT-IR

Synthesis, structural characterization and biological activity of Cu(II), Co(II) and Ni(II) complexes derived from 2-(thiazol-2-ylimino)thiazolidin-4-one ligand

A novel series of metal complexes of 2-(thiazol-2-ylimino) thiazolidin-4-one ligand were prepared; the corresponding ligand was synthesized from reaction 2-Chloro-N-(thiazol-2-yl) acetamide with ammonium thiocyanate. The complexes are characterized by FTIR, UV-Vis, molar conductance and mass spectroscopy. The low molar conductance values indicate that the complexes are non-electrolytes.Spectroscopic studies confirmed that the ligand bonded to the metals through the sulphur atoms. Coordination number of copper and nickel complexes is four with square planar geometry, while the cobalt complex has octahedral geometry.In vitro antibacterial activity of ligand and its metal complexes was evaluated using well diffusion method and compared to the standard drug (tetracycline). The antibacterial activitywas examined against Escherichia coli, and pseudomonas aeruginosa, as gram negative bacteria and Staphylococcus aureus as gram positive bacteria. It was found that Nickel complex has the highest antibacterial activity among the synthesized compounds with Zone inhibition diameter in the range 25-29 mm

Kinetic H/D exchange study of Co(III) coordination compounds of diazines using NMR spectroscopy

The Co(III) diazines complexes having composition (NH3) 5CoPhtz)(ClO4), (1) (Phtz = phthalazine), (NH 3)5CoPydz)(ClO4)3 (2) (Pydz = pyradazine), (NH3)5Co(3-Me-Pydz)(ClO4) 3 (3) (3-Me-Pydz = 3-methyl pyradazine) and (NH3) 5Co(3-MePhtz)(ClO4)3 (4) (3-MePhtz = 3-methyl phthalazine), (NH3)5Co(ImH)(ClO4), (5) (ImH = imidazole), (NH3)5Co(NMeIm)(ClO4) 3 (6) (N-MeIm = N-methylimidazole) undergo OD--catalyzed H/D exchange at the ortho position of the coordinated site. Rate constants for H/D exchange of these complexes at 25°C or 60°C were obtained in alkaline D2O solution using NMR spectroscopy. Reaction rate for (NH3)5CoPhtz)(ClO4)3, (NH 3)5CoPydz)(ClO4)3, (NH 3)5Co(3-MePydz)(ClO4)3 and (NH3)5Co(3-MePhtz)(ClO4)3 at 25°C are faster compared to (NH3)5Co(ImH)(ClO 4)3, (NH3)5Co(N-MeIm)(ClO 4)3 (7). However (NH3) 5CoImCo(NH3)5Br5 complex does not H/D exchange at 60°C even in strong alkaline D2O solution

Synthesis of Some Benzimidazole-substituted Benzotriazoles

2-Alkylsubstituted benzimidazoles (3a–h) were prepared from the acid-catalyzed reaction of 4-methyl-1,2-phenylenediamine with corresponding carboxylic acids. Addition of these benzimidazoles to N-chloromethylbenzotriazole in the presence of sodium amide under reflux conditions gave the novel benzimidazole-substituted benzotriazoles (5a–f). IR and 1HNMR spectroscopy and elemental analysis were used for the identification of these compounds.Keywords: Phenylenediamine, benzimidazole, benzotriazol

One-pot synthesis of tetrahydropyrimidines catalyzed by zeolite

A simple one-pot synthesis of various tetrahydro pyrimidines in the presence of NaY zeolite, as an efficient catalyst, is reported. The multicomponent reaction was carried out by a three-component coupling of 1,3-diketone, aldehyde and urea/thiourea in the presence of the catalyst to give 1(a-k). The catalyst could be reused several times. Further reaction of these pyrimidines with phosphorus oxychloride gave corresponding N-formylated compounds

An Efficient and Convenient Protocol for the Synthesis of Optically Active 1,2,4-Triazolo-[3,4-b]-[1,3,4]-Thiadiazole, 1,3,4-Oxadiazole and 1,3,4-Thiadiazole Derivatives having L-Amino Acid Moieties

A series of novel bis triazolothiadiazole, 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives attached to L-amino acid moieties were synthesized in good yields using a simple and practical method. The structure of all synthesized compounds was confirmed by IR, 1H NMR, 13C NMR spectroscopy and elemental analysis.Keywords: Amino acid, triazolothiadiazole, 1,3,4-oxadiazole, 1,3,4-thiadiazole, phosphorus oxychloride, triazol