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Synthesis and Characterizations of Dipeptide Derivative of Gentamicin
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Abstract

      The target derivative are gentamicin linked with L-Val- L-Ala by an ester linkage. These were synthesized by esterification method, which included the reaction of -OH hydroxyl group on (carbon No.5) of gentamicin with the acid chloride of the corresponding dipeptide, The preparation of new derivative of gentamicin involved protected the primary & secondary amine groups of Gentamicin, by Ethylchloroformate (ECF) to give N-carbomethoxy Gentamicin which was used for further chemical synthesis involving the free hydroxyl groups.

Then prepared dipeptide (L-Val- L-Ala) by conventional solution method in present DCC & HoBt then reacted with thionyl chloride to prepared acid chloride of dipeptides, then after, linked by ester linkage to N-protection gentamicin in present pyridine as base, finally deportation the amino group of synthesized compound by using TFAA in present anisole.

The characterization of the titled compounds were performed utilizing FTIR spectroscopy, CHNS elemental analysis, and by measurements of their physical properties.

 

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Publication Date
Sat Dec 24 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Antimicrobial Activity of Nitrogen-Containing Anthraquinone Derivatives
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New substituted anthraquinones with amino derivations fragments were synthesized through the substitution of bromine atom by different amines using the Ullmann coupling reaction. Obtained compounds based on anthraquinone used for experimental antimicrobial studies. The structure of the synthesized compounds was confirmed by LC-MS and 1H, 13C NMR spectroscopy. Studies on planktonic microorganisms have shown that the first synthesized anthraquinone derivatives have an inhibitory effect against bacteria and fungi. The triazene 1-(3-(benzoic acid(triaz-1-en-1-ol(-4-(1H-imidazol-1-yl(-9,10-dioxo-9,10-dihydroanthracene -2-sulfonic acid, have wide spectrum of activity, growth retardation zones against gram-positive micro

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Publication Date
Thu Mar 19 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives
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The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.

Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses

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Publication Date
Wed Apr 20 2016
Journal Name
Transactions Of Engineering And Sciences
Synthesis and Antibacterial Activities of Some mixed ligand complexes
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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

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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of 2(2-Tetrahydropyranylthio) methyl cyclopropylamine
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2(2-Tetrahydropyranylthio) methyl cyclopropyl amines were synthesized from allylmercaptan through several steps. The structures of the intermediates and the final products where confirmed through IR, NMR and elemental analysis, these compounds may be of value in the treatment of diseases  where free radicals are implicated in their pathogensis, since the thio and the amino groups of the synthesized compounds may act as free radical scavengers.

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Publication Date
Sun May 07 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some Amides Containing Isoxazoline Ring
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This work involves synthesis of amides containing isoxazoline unit starting with
chalcone; 4-[3-(3‾-nitrophenyl)-2-propene- 1-one]-aniline[I]. 4-Aminoacetophenone was
reacted with 3-nitrobenzaldehyde in basic medium giving chalcone [I] by claisen-schemidt
reaction. The chalcone [I] was reacted with hydroxylamine hydrochloride giving isoxazoline
[II] in NaOH basic medium. The amides with structural formula [III]a-h were prepared by the
reaction of amino compounds ; isoxazoline [II] with different acid chlorides in dry pyridine
and using DMF as a solvent at 4
0
C. All the synthesized compounds have been characterized
by melting points , FTIR and
1
HMNR (of compound [III]a) spectroscopy.

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Publication Date
Tue Oct 02 2018
Journal Name
Iraqi Journal Of Physics
Synthesis and characterization of Au nanoparticles for nanomedicine application
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Gold nanoparticles AuNPs have proven to be powerful tools in various nanomedicine applications, because of their photo-optical distinctiveness and biocompatibility. Noble metal gold nanoparticles was prepared by pulsed laser ablation method (1064-Nd: YAG with various Laser power from 200 to 800 mJ and 1 Hz frequency) in distil water. The process was characterized using UV-VIS absorption spectroscopy. Morphology and average size of nanoparticles were estimated using AFM and X-ray diffraction (XRD) analysis which show the nature of gold nanoparticles (AuNPs). Antibacterial activity of gold nanoparticles as a function of particles concentration against gram negative bacterium Escherichia coli and gram positive bacterial Staphylococcus aureu

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Publication Date
Wed Apr 27 2016
Journal Name
Transactions On Engineering And Sciences
Synthesis and Antibacterial Activities of Some mixed ligand complexes
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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

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Publication Date
Sat Jun 19 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Evaluation of Some Coumarin Derivatives
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Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial   antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria  (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr

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Publication Date
Fri Nov 29 2019
Journal Name
Iraqi Journal Of Physics
Synthesis and Characterization of P3HT Metal Nanoparticles Hybrid Junction
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In this work the fabrication and characterization of poly(3-hexylthiophene) P3HT-metallic nanoparticles (Ag, Al). Pulsed Laser Ablation (PLA) technique was used to synthesis the nanoparticles in liquid. The Fourier Transformer Infrared (FTIR) for all samples indicate the chemical interaction between the polymer and the nanoparticles. Scanning Electron Microscopic (SEM) analysis showed the particle size for P3HT-AgNps samples between 44.50 nanometers as well the spherical structure. While for P3HT-AlNps samples was flakes shape. Energy Dispersive X-ray (EDX) spectra show the existing of amount of metallic nanoparticles.

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