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. Metronidazole has a half-life of 6.5 ± 2.9 hours. A number of studies have recently been conducted on the selective substitution of hydrogen with deuterium. which increases the bond strength, increasing the biological half-life and, consequently, the drug's metabolic stability also increases. In an attempt to address metronidazole's drawbacks and clinical resistance, deuterated metronidazole was synthesised, characterised, and tested for antibacterial, antifungal, and anti-tubercular activities. The metronidazole and its deuterated compound showed equipotent antifungal activity and aerobic antibacterial activity. Also, when compared with the non-deuterated compound, deuterated metronidazole exhibited better anaerobic antibacterial and anti-tubercular activity.
A new series of metal ions complexes of VO(II), Cr(III), Mn(II), Zn(II), Cd(II) and Ce(III) have been synthesized from the Schiff bases (4-chlorobenzylidene)-urea amine (L1) and (4-bromobenzylidene)-urea amine (L2). Structural features were obtained from their elemental microanalyses, magnetic susceptibility, molar conductance, FT-IR, UV–Vis, LC-Mass and 1HNMR spectral studies. The UV–Vis, magnetic susceptibility and molar conductance data of the complexes suggest a tetrahedral geometry around the central metal ion except, VOII complexes that has square pyramidal geometry, but CrIII and CeIII octahedral geometry. The biological activity for the ligand (L1) and its Vanadium and Cadmium complexes were studied. Structural geometries of com
... Show MoreIn this research two series of the new derivatives of Trimethoprim and paracetamol drugs have been prepared which known as a high medicinal effectiveness. Series (A) is including the interaction of diazonium salt of trimethoprim and coupling with some substituted phenol compounds (2-amino phenol, 3-ethyl phenol, 1-naphthol, 2-nitro phenol, Salbutamol). Series (B) is including the interaction coupling alkali solution of paracetamol with diazonium salt of some substituted aniline compounds (Benzedine, 2, 3-di chloro aniline, Trimethoprim, Anilinium chloride, 2-nitro- 4-chloro aniline).Chemical structures of all synthesized compounds were confirmed by UV-visible and FTIR spectroscopy.
Antacids have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, gastritis, irritable stomach, gastric and duodenal ulcers. A pH-responsive of bi-polymer of sodium alginate and pectin have been studied as raft-forming polymers using sodium bicarbonate and calcium carbonate as gas-generating and calcium ion sources. The aim of study was to formulate and evaluate mono and bilayer tablets of floating and sustained release antacid delivery systems using sodium carboxy methyl cellulose as a gel forming substance, calcium and magnesium carbonate as sources of acid neutralizing and carbon dioxide gas generators agents upon contact with acidic solution. The effect of the formulation
... Show MoreThe research includes synthesis and identification of novel three amino acids ligands complexes of some heavy metal (II) ions by using the amino acids like glycine, L-alanine and L-valine. New metal mixed ligand complexes with amino acids are prepared the reaction by reacting the three amino acids with the metals(II) chloride by using 50% ethanolic solution and 50% distall water in the molar ratio [1:1:1:1] ( M:Gly:Ala:Val) except for Co(II) and Ni(II) complexes were found after diagnosis the coordination with both Lalanine and L-valine. The prepared complexes identified by using physical properties, flame atomic absorption and conductivity measurements, in addition, mass, FT.IR and UV.vis spectrum as well magnetic moment data. The general
... Show MoreNew compounds containing heterocyclic units have been synthesized. These compounds include 2-amino 5- phenyl-1,3,4-thiadiazole (1) as starting material to prepare the Schiff bases 2N[3-nitrobenzylidene -2 hydroxy benzylidene and 4-N,N-dimethyl aminobenzylidene] -5-phenyl-1,3,4-thiadiazole (2abc) , 2N[3-nitrophenyl, 2-hydroxyphenyl or 4-N,N-dimethylaminophenyl] 3-]2-amino-5-phenyl-1,3,4-thiadiazole]-2,3-dihydro-[1,3]oxazepine-benzo-4,7-dione] (3abc), 2N[3-nitrophenyl,2-hydroxyphenyl,4-N,N-dimethylaminophenyl]-3-[2-amino-5-phenyl-1,3,4-thiadiazole-2-yl]-2,3-dihydro-[1,3]oxazepine-4,7-dione[(4abc), 2-N-[3-nitrophenyl, 2-hydroxyphenyl or 4-N,N-dimethylaminophenyl]-3-[2-amino-5-phenyl-1,3,4-thiadiazole-2yl]-1,2,3-trihydro-benzo-[1,2-e][1,3] diaz
... Show MoreA process of bacterial cellulose gold nanocomposite has been investigated based on experimental work and cited literature. A literature review on the production process is carried out in this study. Bacterial cellulose is a high crystalline fabric material generally used in biomedical applications. A Nanocomposite was made by synthesis from gold and bacterial cellulose. The experimental work includes growing, and isolating bacterial cellulose, preparation of gold Nanoparticles and preparation of Nano composite. Nanoparticle’s formation and adsorption on the cellulose tissue have been observed visually, where a colour change was observed. The predicted particle size for the gold nano
Some new heterocyclic compounds containing, cyclohexenone, indazole, isoxazoline, pyrmidine and pyrazoline ring system were prepared from chalcones (1a,b). The starting chalcones (1a,b) were obtained by a base catalyzed condensation of appropriately substituted benzaldehydes and 2-acetylbenzofuran. The reaction of the prepared chalcones with ethylacetoacetate/hydrazine hydrate, hydroxylamine hydrochloride, urea, thiourea, hydrazine hydrate, phenyl hydrazine or hydrazide derivatives gave the mentioned heterocycles. All synthesized compounds have been characterized by physical and spectral methods.
New complexes of M(II) with mixed ligand of 5-Chlorosalicylic acid (CSA) C7H5ClO3 as primary ligand and L- Valine (L-Val) C5H11NO2 as a secondary ligand were prepared and characterized by elemental analysis (C.H.N), UV., FT-IR, magnetic susceptibility, μeff (B.M) as well as the conductivity measurements (Λm ). In the complexes, the 5-chlorosalicylic acid is bidentate in all complexes coordinating through –OH- and –COO- groups; also L-Valine behaves as a bidentate ligand in all complexes through –NH2 and –COO- groups. These five mixed ligand complexes formulated as Na3[M(CSA)2(L-Val)]. The proposed molecular structure for all complexes is octahedral geometries. The synthesis complexes were tested in vitro for against four bacteria
... Show MoreThe synthesis of conducting polyaniline (PANI) nanocomposites containing various concentrations of functionalized single-walled carbon nanotubes (f-SWCNT) were synthesized by in situ polymerization of aniline monomer. The morphological and electrical properties of pure PANI and PANI/SWCNT nanocomposites were examined by using Fourier transform- infrared spectroscopy (FTIR), and Atomic Force Microscopy (AFM) respectively. The FTIR shows the aniline monomers were polymerized on the surface of SWCNTs, depending on the -* electron interaction between aniline monomers and SWCNTs. AFM analysis showed increasing in the roughness with increasing SWCNT content. The AC, DC electrical conductivities of pure PANI and PANI/SWCNT nanocomposite h
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