This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in dry pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [2-amino-5-mercapato-1,3,4-thiadiazole] was prepared through the reaction of thiosemicarbazide with carbon disulphide (CS2) in entity of anhydrous (Na2CO3) in (abs. ethanol ). Compound (VI) [2-(5-mercapto-1,3,4-thiadiazol-2-yl)isoindoline-1,3-dione] was synthesized by the reaction of phthalic anhydride with compound (V) in presence of (gla. CH3COOH). Reaction of compound (VI) with (ClCH2COOH) in entity of anhydrous (Na2CO3) in distilled water produced compound (VII) and then reaction with thionyl chloride yielded acid chloride (VIII). Condensation of acid chloride with hydrazine hydrate afforded 2-(5-(1,3-dioxoisoindolin-2-yl)-1,3,4-thiadiazol-2-ylthio)acetohydrazide (IX). The azomethine (X) has been synthesized from the reaction between compounds (IX) and (IV). Moreover compounds (XI-XIII) were synthesized from the cyclic condensation of Schiff base (X) with (maleic, phthalic and 3-nitrophthalic) anhydride, the structures of the novel synthesized compounds have been confirmed by physical properties and spectral measurements such as (FTIR and some of them by 1H-NMR and 13C-NMR).
ABSTRACT: Oxadiazole ring is a heterocyclic molecule with an oxygen and two nitrogen atoms spread throughout its five-membered structure. There are four different isomers that have been discovered, Because of their wide applications in a range of sectors, including medications . Some of these biological activity are; anticonvulsant capacity, anticancer as well, antibacterial, antiviral, antifungal, antimalarial, antitubercular, anti-asthmatic, antidepressant, antidiabetic, antioxidant, antiparkinsonian, analgesic and anti-inflammatory, are just some of the therapeutic uses that have drawn attention to drug candidates containing an oxadiazole moiety. This review, we will examine the various methods of oxadiazole synthesis. The mo
... Show MoreIn this work, of New Ligand [(E)-5-hydroxy-4-(3-(4-methoxy phenyl) acryl amido) naphthalene -1- sulfonic acid] (ANS) was prepared by reflexing reaction of 4-amino-5-hydroxy naphthalene sulfonic acid with para methoxy cinnamic acid, this produced and described chemical was employed as ligand to prepare tri and di-organotin complexes by condensation reaction with the salts of organotin chloride (phenyl, butyl, and methyl tin chloride). Specialized methods, including elemental analysis, (tin and proton) magnetic resonance, and infrared spectra, were used to identify the complexes. DPPH (2,2-diphenyl-1-picrylhydrazyl) and CUPRAC (Cupric Reducing Antioxidant Capacity) are both commonly used methods for measuring antioxidant capacity in v
... Show MoreIn this work, an important sugar alkynyl ether has been synthesized in two subsequent steps starting from commercially available D-galactose (3). This kind of compounds is highly significant in the synthesis of biologically active molecules such as 1,2,3-triazole and isoxazoles. In the first step, galactose (3) was reacted with acetone in the presence of anhydrous copper (II) sulfate to produce 1,2:3,4-di-O-isopropylidene-α-D-galactose (4) in good yield. The latter was reacted with excess of 3-bromoprop-1-yne in DMF in the presence of NaOH pellets to afford the target molecule 5 in a very good yield. The temperature of this step is crucial in determining the reaction yi
... Show MoreSchiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacter
... Show MoreBackground: Meclizine hydrochloride (MCZ) is an antihistamine that is used as an antiemetic to prevent and cure nausea and vomiting. Because of its limited water solubility and first-pass metabolism, it exhibits variable absorption. Objective: To formulate and evaluate MCZ as an intranasal in situ gel with increased residence time and permeability. Methods: We made an inclusion complex of MCZ using various cyclodextrins as a complexing agent to help the drug dissolve better. The complexes were studied, and the ones that were better at dissolving were chosen to be used in the creation of an in situ gel with poloxamer 407 (17–20% w/v) and hyaluronic acid (0.25–0.75% w/v). Prepared formulas were subjected to various evaluation tes
... Show MoreEthanol as a solvent, a precursor of titanium isopropoxide and a stabilizer of either hydrochloric acid or ammonium hydroxide was used to prepare a titanium dioxide aqueous solution. The aqueous solutions with different values of pH and the morphology of the resultant reaction of the nanoparticles of titanium dioxide were investigated. The X-ray diffraction showed that at low temperatures and with acidic solutions, rutile structures are more favorable to grow on titanium dioxide synthesized, while at low and average temperatures and with base solutions, anatase phase is more pronounced. The crystalline form and the re-confirmation of the crystallite size growth were observed by the scanning electron microscopy. The atomic force micr
... Show Moreby in situ polymerization of aniline monomer, conducting polyaniline (PANI) nanocomposites containing various concentrations of carboxylic acid functionalized multi-walled carbon nanotubes (f-MWCNT) were synthesized. The morphological and electrical properties of pure PANI and PANI /MWCNT nanocomposites were examined by using Fourier transform- infrared spectroscopy (FTIR), X-ray diffraction (XRD) and Atomic Force Microscopy (AFM) respectively. FTIR spectra shows that the carboxylic acid groups formed at the both ends of the sidewalls of the MWCNTs. The aniline monomers were polymerized on the surface of MWCNTs, depending on the -* electron interaction between aniline monomers and MWCNTs and hydrogen bonding into interaction between t
... Show MoreEthanol as a solvent, a precursor of titanium isopropoxide and a stabilizer of either hydrochloric acid or ammonium hydroxide was used to prepare a titanium dioxide aqueous solution. The aqueous solutions with different values of pH and the morphology of the resultant reaction of the nanoparticles of titanium dioxide were investigated. The X-ray diffraction showed that at low temperatures and with acidic solutions, rutile structures are more favorable to grow on titanium dioxide synthesized, while at low and average temperatures and with base solutions, anatase phase is more pronounced. The crystalline form and the re-confirmation of the crystallite size growth were observed by the scanning electron microscopy. The atomi
... Show MoreIn this review, previous studies on the synthesis and characterization of the metal Complexes with paracetamol by elemental analysis, thermal analysis, (IR, NMR and UV-Vis (spectroscopy and conductivity. In reviewing these studies, the authors found that paracetamol can be coordinated through the pair of electrons on the hydroxyl O-atom, carbonyl O-atom, and N-atom of the amide group. If the paracetamol was a monodentate ligand, it will be coordinated by one of the following atoms O-hydroxyl, O-carbonyl or N-amide. But if the paracetamol was bidentate, it is coordinated by atoms (O-carbonyl and N-amide), (O-hydroxyl and N-amide) or (O-carbonyl and O-hydroxyl). The authors also found that free paracetamol and its complexes have antimicrobial
... Show More