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Synthesis, Characterization and Study Biological Activity of Some New 1, 3, 4-Thiadiazole and Pyrazolone Derivatives Containing Indole Ring
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This work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring. The new 2-amino-1, 3, 4-thiadiazole derivatives [IV] and [V] a, b were synthesized by cyclization reaction of 2-methyl-1H-indole-carbothiosemicarbazide [III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2-amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone derivatives [XI] a, b were synthesized from heating under reflux equimolar from a mixture of acid hydrazides [X] a or [X] b and ethylacetoacetate in absolute ethanol. Acetyl pyrazolone compounds [XII] a, b were synthesized by the reaction of pyrazolone derivatives [X] a or [X] b with acetyl chloride in 1, 4-Dioxane in present of calcium hydroxide to give 4-acetyl pyrazolone derivatives [XI] a, b. The new aryl hydrazone derivatives of pyrazoline [XIII] and [XIV] were synthesized by the reaction of one mole of compounds [XII] a or [XII] b with one mole of phenyl hydrazine or substituted phenyl hydrazine in ethanol. All the synthesized compounds have been characterized by melting points, FTIR, 1HNMR and Mass spectroscopy

Publication Date
Thu Oct 03 2024
Journal Name
Applied Organometallic Chemistry
Synthesis, Characterization, Molecular Docking, Cytotoxicity, and Antimicrobial Activity of Schiff Base Ligand and Its Metal Complexes
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ABSTRACT<p>A Schiff base ligand (L) was synthesized via condensation of <italic>N</italic>‐(1‐naphthyl)ethylenediamine dihydrochloride with phthalaldehyde. The ligand was characterized by FT‐IR, UV–Vis, <sup>1</sup>H NMR, mass spectrometry, and elemental analysis (C, H, N). Five metal complexes (Co(II), Ni(II), Cu(II), Zn(II), and Cd(II)) were prepared with the ligand in a 1:1 (M:L) ratio using an aqueous ethanol solution. The complexes were characterized by FT‐IR, UV–Vis, mass spectrometry, and elemental analysis (C, H, N). Additionally, <sup>1</sup>H NMR spectroscopy was employed for Cd(II) complex. Antimicrobial activity of the ligand and its metal complexes against </p> ... Show More
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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Characterization of Biodegradable Microspheres Containing Sertraline Hydrochloride
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Four batches of sertraline HCl microspheres were prepared using a poly (D-L-lactide-co-glycolide) (PLGA) polymer ( Mw. 9, 27, 30 and 83 KDa) as  a delivery system. The microspheres were prepared by a dispersion/solvent extraction-evaporation method and characterized for drug loading by UV, particle size by laser diffractometry and surface morphology by scanning electron microscopy (SEM). The in vitro sertraline HCl release was studied. Spherical microspheres with a mean diameter of 21 to 26 µm loaded with 24.6 – 38.2% were produced. The in vitro drug release was shown to be depend on polymer molecular weight and also on the drug loading. Differential scanning calorimetry (DSC) was employed to investigate the physical state

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Publication Date
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Synthesis, characterization, molecular docking, ADMET prediction, and anti-inflammatory activity of some Schiff bases derived from salicylaldehyde as a potential cyclooxygenase inhibitor
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A series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these

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Publication Date
Mon Aug 01 2022
Journal Name
Baghdad Science Journal
Preparation, Spectroscopy, Biological Activities and Thermodynamic Studies of New Complexes of Some Metal Ions with 2-[5-(2-Hydroxy-Phenyl)- 1,3,4-Thiadiazol-2-Ylimino]-Methyl-Naphthalen-1-Ol]
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This study describes the preparation of new series of tetra-dentate N2O2 dinuclear complexes (Cr3+, Co2+, Cu2+) of the Schiff base derived from condensation of 1-Hydroxy-naphthalene-2-carbaldehyde with 2-amino-5-(2-hydroxy-phenyl)-1,3,4-thiadiazole. The structures of the ligands were identified using IR, UV-Vis , mass,  elemental analysis and 1H-NMR techniques. All prepared complexes have been characterized by conductance measurement, magnetic susceptibility, electronic spectra, infrared spectrum, theromgravimatric analysis (TGA) and metal analysis by atomic absorption. From stoichiometry of metal to ligand and all measurements show a octahedral geometry proposed for all complexes of the (Cr3+, Co2+, Cu2+). conductivity measurement shows t

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Publication Date
Mon Aug 01 2022
Journal Name
Baghdad Science Journal
Preparation, Spectroscopy, Biological Activities and Thermodynamic Studies of New Complexes of Some Metal Ions with 2-[5-(2-Hydroxy-Phenyl)- 1,3,4-Thiadiazol-2-Ylimino]-Methyl-Naphthalen-1-Ol]
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This study describes the preparation of new series of tetra-dentate N2O2 dinuclear complexes (Cr3+, Co2+, Cu2+) of the Schiff base derived from condensation of 1-Hydroxy-naphthalene-2-carbaldehyde with 2-amino-5-(2-hydroxy-phenyl)-1,3,4-thiadiazole. The structures of the ligands were identified using IR, UV-Vis , mass,  elemental analysis and 1H-NMR techniques. All prepared complexes have been characterized by conductance measurement, magnetic susceptibility, electronic spectra, infrared spectrum, theromgravimatric analysis (TGA) and metal analysis by atomic absorption. From stoichiometry of metal to ligand and all measurements show a octahedral geometry proposed for all

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Publication Date
Sat Sep 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of some 1,3-diazepine -4,7-diones derivatives (part 2)
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1,3-0xazepine-4)-diones were  prepared by c.ondensation of N­

cinnamylideneareneamines with maleic anhydride,  phthalic;; anhydride

,and  3-nitrophthalic  anhydride.  The  oxazepjne::; were  reacted  with

primary aromatic  amine  to give the corresponding  1 ,3--diazepine-4,7- diones.

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design and Synthesis of Some Nitrate Derivatives of Mefenamic Acid with Expected Nitric Oxide Release
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This study include design and synthesis of 2 derivatives of compounds consisting of mefenamic acid, glycine and organic nitrates (2-nitrooxy ethanol or 1,3-dinitrooxy-2-propanol). Nitric oxide NO has been reported to support many of the same mucosal protection mechanisms as prostaglandins and is sufficient for acute gastroprotection and ulcer healing. So we suppose these 2 compounds would reduce non-steroidal anti-inflammatory drugs NSAIDs gastrointestinal side effect.

Key words: Non-Steroidal anti-inflammatory dr

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Publication Date
Mon Feb 20 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Transition Metals Ions Complexes with 2-Thioxoimidazolidin-4-One Schiff Base as Ligand
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Mn(II), Co(II), Ni(II), Cu(II), and Cr(III) metal complexes with the ligand (L) [3-(2nitro benzylidene) amino-2-thioxoimidazolidin-4-one] have been prepared and characterized in their solid state using the elemental micro analysis (C.H.N.S), flame atomic absorption, UV-Vis spectroscopy, FT-IR, magnetic susceptibility measurements, and electrical molar conductivity. The ratio of metal to ligand [M:L] was got for all complexes in the ethanol by using the molar ratio method, which produced comparable results with those results obtained for the solid complexes. From the data of all techniques, octahedral geometry was proposed for Cr(III), Mn(II), and Co(II) complexes, while tetrahedral structure was proposed for Ni(II), Cu(II) complexes.

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Biological activity and protease inhibitor from watery extract of lentil (Lens culinaris) against some bacterial species
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Biological activity substances was investigated in watery extract of lentil which found to contain phenols, tannin, saponins and resins while, flavons, terpens and steroids were not exist in the extract details explained that 5%, 10% of lentil extract largly inhibited the growth of Psedumonas aeruginosa then Escherichia coli and Bacillus subtilis. The growth of both Staphylococcus aureus and Salmonella typhimurium were slightly affected by all extract concentration. Extracellular protease were screened in all bacterial species under study. Complete inhibition was achieved for extracellular protease while different percentage of protease inhibition were seen for intracellular proteases.

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Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Synthesis and characterization of some mixed ligands complexes of β-enaminone with some metal ions
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