Synthesis, Characterization And Biological Evaluation of Schiff Base And Ligand Metal Complexes of Some Drug Substances
In the present study a series of some four-,five-and seven-membered heterocyclic compounds have been synthesized by the reaetion of Schiff bases (1a,b) with chloroacetyl chloride, sodium azide, thioglycolic acid or various anhydrides to give azetidinone (2a,b), tetrazole (3a,b), thiazolidinone (4a,b) and 1,3-oxazepine derivatives (5-8a,b) respectively. Schiff bases (1a,b)were prepared from the reaction of p-toluidine with aromatic aldehydes. All synthesized compounds were characterized by physical properties and spectral data.
In this study, the preparation and characterization of hyacinth plant /chitosan composite, as a heavy metal removal, were done. Water hyacinth plant (Eichhorniacrasspes) was collected from Tigris river in Baghdad. The root and shoot parts of plant were ground to powder. Composite materials were prepared at different ratios of plant part (from 2.9% to 30.3%, wt /wt) which corresponds to (30-500mg) of hyacinth plant (root and shoot) and chitosan. The results showed that all examined ratios of plant parts have an excellent absorption to copper (Cu (II)). Moreover, it was observed that 2.9% corresponds (30mg) of plant root revealed highest removal (82.7%) of Pb (II), while 20.23% of shoot removed 61% of Cd (II) within 24 hr
... Show MoreSelexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MoreBackground: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MoreThe compound 3-[4Ì„-(4Ë-methoxy benzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one [III] was prepared from the cyclization of thiosemicarbazone [II] with
ethyl α -chloroacetate in the presence of fused sodium acetate. Treatment the later compound
with acetic anhydride yielded the corresponding 1-Acetyl-3-[ 4Ì„- (4Ë- methoxy benzoyloxy)
benzylideneamino] – 2 – thioxo -imidazolidine-4-one [IV]. 1,3-Oxazepine derivatives [V]a-d
and [VI]a-d are obtained from the reaction of compounds[III] and [IV] with different acid
anhydrides, in dry benzene. The FTIR and
1
HNMR spectroscopy are indicated a good
evidence for the formation of the synthesized compounds. Some of the synthesized
The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met
... Show MoreABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity
... Show MoreA New ligand, N-(2-oxo-1,2- Dihydropyrimidin-4- ylcarbamothioyl) Acetamide (DPA) was prepared by reaction of iso thiosyanate derivative with Cytosine. The ligand has been characterized through elemental analysis, H1 NMR, C13NMR, FT-IR, and UV Visible spectra, such ligand’s transition metal complexes have been characterized through conductivity measurement, FT-IR, UV Visible spectra and magnetic susceptibility, all the complexes of this ligand are solid crystal and molar ratio (2:1) (ligand: metal). The form of molecular for these complexes octa hedral. The general formula [M(DPA)2Cl2], where M+2 = (Mn, Co, Ni, Cu, Zn, Cd, Hg).
In this work, synthesized N4,N4`-bis(2, 3, 4 nitro benzylidene) biphenyi-4-4`-diamine(B1-B3) , was tested as an inhibitors in controlling the corrosion of carbon steel in NaCl 3.5% solution by using open circuit potential (OCP),at four different temperatures (293, 303, 313 and 323 K). Furthermore, the surface morphology was investigated using the Atomic force microscopy (AFM). The effect of using different Schiff bases and temperature was also investigated. Schiff bases was synthesized and characterized via using. Fourier Transform Infrared Spectroscopy (FT-IR)and Atomic Force Microscope (AFM) characterized . The experimental results shown that Schiff bases can consider as an excellent corrosion inhibitors for carbon steel in NaCl 3
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