Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 144-fold increase in aqueous solubility compared to ciprofloxacin. Taste evaluation by panel method showed palatable taste in prodrugs compared to the parent drugs. The synthesized compounds were screened for their antimicrobial activity against different bacterial strains which are, Staphylococcus aureus, Pseudomonas aeruginosa, E. coli and Klebsiella pneumonia. The prodrugs have revealed excellent antibacterial activities compared with the parent compounds. Chemical hydrolysis study at pH (1.2 and 7.4) has indicated that these compounds may pass unhydrolyzed through the stomach and produce enough stability to be absorbed from the intestine as indicated by t1/2 values.
New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hy
... Show MoreNew series of 4, 4'-((2-(Aryl)-1H-benzo [d] imidazole-1, 3 (2H)-diyl) bis (methylene)) Diphenol (3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr
... Show MoreIn this work, we study the effect of doping Sn on the structural and optical properties of pure cadmium oxide films at different concentrations of Tin (Sn) (X=0.1,0.3 and 0.5) .The films prepared by using the laser-induced plasma at wavelength of laser 1064 nm and duration 9 ns under pressure reached to 2.5×10-2 mbar. The results of X-ray diffraction tests showed that the all prepared films are polycrystalline. As for the topography of the films surface, it was measured using AFM , where the results showed that the grain size increases with an increase in the percentage of doping in addition to an increase in the average roughness. The optical properties of all films have also been studied through the absorbance s
... Show MoreMixed ligand complexes of bivalent metal ions, viz; Co(II), Ni(II), Cu(II) and Zn(II) of the composition [M(A)2((PBu3)2]in(1:2:2)(M:A:(PBu3). molar ratio, (where A- Anthranilate ion ,(PBu3)= tributylphosphine. M= Co(II),Ni(II),Cu(II) and Zn(II). The prepared complexes were characterized using flame atomic absorption, by FT-IR, UV/visible spectra methods as well as magnetic susceptibility and conductivity measurements. The metal complexes were tested in vitro against three types of pathogenic bacteria microorganisms: (Staphylococcus, Klebsiella SPP .and Bacillas)to assess their antimicrobial properties. Results. The study shows that all complexes have octahedral geometry; in addition, it has high activity against tested bacteria. Based on th
... Show MoreThe current work reports a new Schiff base [N1-benzylidenebenezene-1,2-diamine(L) = C20H16N2] has been synthesized from benzaldehyde (C6H5CHO) and O- aminoaniline (O-C6H4(NH2)2. Metal mixed ligand complexes of the Schiff base were prepared from chloride salts of Zn(II), Cd(II) and Hg(II) in ethanol and 8-hydroxyquinoline(8HQ)(C9H7NO) containing sodium hydroxide. All the complexes were characterized on the basis of their; FT-IR and U.V spectra, melting point, molar conductance, and determination of the percentage of the metal in the complexes by flame (AAS). In the all complexes, (8HQ) behaves as a bidentate ligand as primary ligand through –-OH phenolic group and –N groups of pyridine group. Also, the prepared ligand (L) was bidentate i
... Show MoreComplexes of Co(II),Ni(II),Cu(II)and Zn(II) with mixed ligand of 4- aminoantipyrine (4-AAP) and tributylphosphine (PBu3) were prepared in aqueous ethanol with (1:2:2) (M:L:PBu3). The prepared complexes were characterized using flame atomic absorption, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. In addition biological activity of the two ligands and their complexes against three selected type of bacteria were also examined. The general compositions of the complexes are found to be [M(4-AAP)2(PBu3)2] Cl2 . Where M= Co(II),Ni(II),Cu(II)and Zn(II). Some of the complexes exhibit good bacterial activities. From the obtained data the octahedral structures have suggested for all prepare
... Show MoreNew metal complexes of the ligands 2-benzamido benzothiazole(B1), and 2-actamido benzothiazole(B2) with metal ions Ni(II),and Co(II) were prepared in alcoholic medium. The prepared complexes were characterized by FT-IR and electronic spectroscopy, Magnetic susceptibility, Flame Atomic Absorption technique as well as elemental analysis and conductivity measurement. From the spectral studies, an octahedral monomer structure proposed for Ni(II) complexes, and a tetrahedral monomer structure for Co(II)complexes.Semi-empirical methods (PM3,and ZINDO/1)were carried out to evaluate the heat formation( ?H?f)binding energy(?Eb) and dipole moment(µ)for all metal complexes. Also vibration frequencies, Electrostatic potential, HOMO and LUMO
... Show MoreMixed ligand complexes of bivalent metal ions, viz; Co(II), Ni(II), Cu(II) and Zn(II) of the composition [M(A)2((PBu3)2]in(1:2:2)(M:A:(PBu3). molar ratio, (where A- Anthranilate ion ,(PBu3)= tributylphosphine. M= Co(II),Ni(II),Cu(II) and Zn(II). The prepared complexes were characterized using flame atomic absorption, by FT-IR, UV/visible spectra methods as well as magnetic susceptibility and conductivity measurements. The metal complexes were tested in vitro against three types of pathogenic bacteria microorganisms: (Staphylococcus, Klebsiella SPP .and Bacillas)to assess their antimicrobial properties. Results. The study shows that all complexes have octahedral geometry; in addition, it has high activity against tested bacteria. Based on th
... Show MoreMixed ligand metal complexes of CrIII, FeIII,II, NiII and CuII have been synthesized using 5-chlorosalicylic acid (5-CSA) as a primary ligand and L-Valine (L-Val) as secondary ligand. The metal complexes have been characterized by elemental analysis, electrical conductance, magnetic susceptibility measurements and spectral studies. The electrical conductance studies of the complexes indicate their electrolytic nature. Magnetic susceptibility measurements revealed paramagnetic nature of the all complexes. Bonding
The aim of this work is to produce samples from Iraqi raw materials like Husyniat Bauxite (raw and burnt) and to study the effect of some additives like white Doekhla kaolin clays and alumina on that material properties were using sodium silica as a binding material. Five mixtures were prepared from Bauxite (raw and burnt) and kaolin clays, with an additive of (40) ml from sodium silica and alumina of (2.5, 5, 7.5,10 wt %) percentage as a binding material. the size grading was through sieving. The formation of all specimens was conducted by a measured gradually semi-dry pressing method under a compression force of (10) Tons and humidity ratio ranging from (5-10) % from mixture weight. Drying all specimens was done and then they were burn
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