scholarly journals Synthesis, Biological Activity of Trimethoprim derivative and the Complexes

2021 ◽  
Vol 2063 (1) ◽  
pp. 012014
Author(s):  
Hassan H Albahadly ◽  
Nahed H Al-Haidery ◽  
Bushra K Al-Salami

Abstract This study demonstrates the synthesis of new ligands derived from trimethoprim with their Iron(III) and copper (ll) complexes. At the beginning, preparing new ligands, the first namly N, N’-(5-(3,4,5-trimethoxybenzyl)pyrimidine-2,4-diyl)bis(3,4,5-trihydroxy benza mide)and the Ligand second namly N, N’-(((5-(3,4,5-trimethoxybenzyl)pyrimidine-2,4-diyl) bis(azanediyl))bis(carbonthioyl) bis(3,4,5-trihydroxybenzamide) which prepared by nucleophilic addition of trimethoprim to Gallic chloride and prepared also by nucleophilic addition of trimethoprim to the Solution of Ammonium thiocyanate and Gallic chloride. Ferric Ion (III) and Copperic Ion (ll) complexes have been prepared with molar ratio [1:2]. The synthesis ligands have been characterized by Uv-Visible, FT-IR, 1HNMR, 13CNMR and EI-mass, while the complexes have been characterized by elemental analysis, Uv-Visible, FT-IR, Conductivity measurements and thermogravemtric (TgA) analysis. The ligands acts as multiple sites coordinating with ferric ion and copper ion, Via lone pair of nitrogen atom of NHC= and phenolic oxygen. In Vitro, the ligands and complexes have been tested for their growth Inhibitory activity against Gram negative bacteria Salmonella Spp and Gram Positive Staphylococcus Spp. The results of the test indicate that the synthesized compounds possessed a high inhibition effectiveness comparative with trimethoprim.

2013 ◽  
Vol 10 (3) ◽  
pp. 954-964
Author(s):  
Baghdad Science Journal

Mefenamic acid was esterified with starchwith[1:1] Molar ratio, as drug substituted with natural polymer, to prolongthe period of hydrolysis of drug polymer with other advantages. The new prodrug starch was characterized by FT-IR and UV-Visible and 1H-NMR spectroscopies. The physical properties were studied and controlled drug release was studied in different pH values at 37oC. The stability of drug was carried out by measuring the absorbance of mefenamic starch which hydrolyzed in HCl solution of pH 1.1 (artificial gastric fluid) and phosphate buffer of pH 7.4 (simulating intestinal fluid SIF) at 37oC for several days. The thermal analysis such as DSC was studied.


2019 ◽  
Vol 17 (72) ◽  
pp. 129-138
Author(s):  
Yasmine Kadom. Al-Majedy

Novel Quinozolins were synthesized in a good yield through convert lacton to lactam and study the biological activity of the synthesized compounds. Quinozolins were characterized by elemental analysis, FT-IR and UV/visible spectra. The novel Quinozolins have been tested in vitro against (gram positive bacteria Staphylococcus aureus and against other gram negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus vulgaris; in order to assess their antimicrobial properties. Moreover, charge, bond length, bond angle, twist angle, heat of formation and steric energy were calculated by using of the ChemOffice program. The study indicates that these Quinozolins have high activity against tested bacteria. Based on the reported results, it may be concluded that the coumarin act as synthons for synthesis of new Quinozolins derivatives through the replacement of oxygen atom by nitrogen atom.


2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Ruijun Wang ◽  
Yunfei Ji ◽  
Ying Peng ◽  
Xiaobo Li

Sijunzi decoction (SJZD) is a classical herbal prescription in traditional Chinese medicine (TCM) used for enhancing the function of immune system. In previous studies, a polysaccharide fraction S-3 was screened from SJZD by assessment of immune system regulation, intestinal microbiota, and SCFA in order to explore the immune active ingredients in SJZD. In the present study, S-3 was further purified, and a homogeneous polysaccharide S-3-1 with a molecular mass of 13.5 × 104 Da was obtained after further fractionation by Sephadex G-150 size-exclusion chromatography. The immunological activities of S-3-1 were assayed in vitro for the first time. The determination of the anticomplement activity showed that S-3-1 displayed inhibitory effects on classical pathway of the complement system, with CH50 values of 530 μg/mL. The FT-IR analysis showed that S-3-1 had absorptive peaks characteristic of polysaccharides. The methylation and GC-MS analysis showed that it is comprised of Rha, Ara, Xyl, Man, Gal, and Glc in a relative molar ratio of 0.35 : 0.37 : 1.4 : 0.31 : 3 : 0.8 and that it mainly contained 1,4-linked-Glc and 1,6-linked-Gal glycosidic bonds. The morphology of S-3-1 was observed by atomic force microscope (AFM). These results provided evidences for tracking the material basis of SJZD immune activity.


2020 ◽  
Vol 13 (2) ◽  
pp. 29-37
Author(s):  
Anilkumar Ambala ◽  
Ch. Abraham Lincoln

A series of novel (E)-2-((Tetrazolo[1,5-a]quinolin-4-ylmethylene)amino)phenol Cu(II), Co(II), Ni(II), Zn(II) and Mn (II) metal complexes have been synthesized 1:1 metal to ligand ratio, and these complexes were characterized by using analytical data such as FT-IR, UV-visible, Mass spectroscopy, SEM, EDX, TGA and magnetic moment measurements. The ligand and all the metal complexes were tested in vitro antimicrobial activity and DNA cleavage studies.


2021 ◽  
Vol 11 (1) ◽  
pp. 3249-3260

Herein, we describe the synthesis and characterization of a Schiff base ligand (E)-N'-(2-hydroxybenzylidene)-4-methoxybenzohydrazide (HBMB) and its Mn(II), Ni(II), and Cu(II) metal complexes (C1-C3) respectively. The ligand HBMB was synthesized by reacting condensation of salicylaldehyde and 4-methoxy benzohydrazide in a 1:1 molar ratio. The structure of HBMB and its metal complexes (C1-C3) were evaluated by using UV-Vis, FT-IR, 1H-NMR, mass spectroscopy as well as on the basis of elemental analysis, conductivity measurements, and thermogravimetric techniques (TGA). The synthesized molecules' tumoricidal properties were performed against human breast cancer (MCF-7) and colon cancer (HT 29) cell lines. The biological results indicated that the ligand, HBMB, and metal complexes possess dose-dependent selective cytotoxicity against the tested carcinoma cells. The synthesized compounds were further evaluated for their in vitro antimicrobial activities against Gram-positive bacteria (Staphylococcus aureus), Gram-negative bacteria (Escherichia coli), and fungal strains (Aspergillus niger).


2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
C. Mallikarjunaswamy ◽  
D. G. Bhadregowda ◽  
L. Mallesha

Pyrimidine salts such as 2-methyl-5-nitro-phenyl-(4-pyridin-3-yl-pyrimidin-2-yl)-amine (1) and 4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-yl-amino)-phenyl-amine (2) with chloranilic and picric acids were synthesized, and theirin vitroantibacterial and antifungal activities were evaluated. The synthesized compounds were characterized by elemental analyses, UV-visible, FT-IR, and1H NMR spectral studies. Compound2aexhibited good inhibition towards antimicrobial activity compared to the other compounds.


2019 ◽  
Vol 31 (8) ◽  
pp. 1871-1876
Author(s):  
Eida S. Al-Farraj ◽  
Amani S. Alturiqi ◽  
Murefah M. Anazy ◽  
Reda A. Ammar

A novel Co(III) complex derived from hexaadentate Schiff base ligand, H3L was described. The ligand is prepared from the reaction of tris-2-aminoethyl amine and o-vanillin in 1:3 molar ratio. The structure of the ligand and its Co(III) complex was described by micro-analyses, FT-IR, NMR, ESI-MS and UV/visible and thermal stability. DFT study was carried out to get insights into the ligand and its Co(III) complex to compare the values of bond lengths and angles with each other. The electronic spectra, Mulliken atomic charge distribution, HOMO-LUMO energy and the thermodynamic parameters have been calculated.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Yasir Arafat ◽  
Saqib Ali ◽  
Saira Shahzadi ◽  
Muhammad Shahid

Heterobimetallic complexes of Zn(II) and Sn(IV) with sarcosine have been synthesized at room temperature under stirring conditions by the reaction of sarcosine and zinc acetate in 2 : 1 molar ratio followed by the stepwise addition of CS2and organotin(IV) halides, where R = Me,n-Bu, and Ph. The complexes were characterized by elemental analysis, FT-IR and NMR (1H,13C) spectroscopy. IR data showed that the ligand acts in a bidentate manner. NMR data revealed the four coordinate geometry in solution state.In vitroantimicrobial activities data showed that complexes (3) and (4) were effective against bacterial and fungal strains with few exceptions.


Author(s):  
W. A. Osunniran ◽  
Y. O. Ayipo ◽  
M. A. Adeyemo ◽  
A.T. Bale ◽  
J. A. Obaleye

Mechanosynthesis and solvent – based syntheses of transition metals (Ni, Co and Zn) complexes of Sodium diclofenac has been carried out by 1:1 molar ratio of the ligand to metal salts respectively. The synthesis of the metal complexes were confirmed by melting point determination, FT-IR (Fourier Transform Infra-red) and UV-visible spectroscopies. The ligand showed bidentate coordination to the metal ions through carboxylate moiety. Octahedral geometry was proposed for all the metal complexes. The antioxidant property of metal complexes was determined using DPPH (1,1-diphenyl-2-picrylhydrazyl) assay with Ascorbic acid as control. The antioxidant evaluation results revealed that the synthesized metal complexes are promising antioxidant agents.


2021 ◽  
Vol 18 (4(Suppl.)) ◽  
pp. 1545
Author(s):  
Anaam M. Rasheed ◽  
Sinan M. M. Al-Bayati ◽  
Dr.Rehab A.M. Al-Hasani ◽  
Muna Ali Shakir

Two Schiff bases, namely, 3-(benzylidene amino) -2-thioxo-6-methyl 2,5-dihydropyrimidine-4(3H)-one (LS])and 3-(benzylidene amino)-6-methyl pyrimidine 4(3H, 5H)-dione(LA)as chelating ligands), were used to prepare some complexes of Cr(III), La(III), and Ce(III)] ions. Standard physico-chemical procedures including metal analysis M%, element microanalysis (C.H.N.S) , magnetic susceptibility, conductometric measurements, FT-IR and UV-visible Spectra were used to identify Metal (III) complexes and  Schiff bases (LS) and (LA). According to findings, a [Cr(III) complex] showed six coordinated octahedral geometry, while [La(III), and Ce(III) complexes]were structured with coordination number seven.  Schiff's bases and mineral complexes were examined in vitro to investigate potential inhibition against Gram-positive bacteria such as Pseudonomous aerugionosa and Gram-negative bacteria such as Staphylococcus aureus. The low concentration for inhibition has been also determined by studying the minimal inhibitory concentrations MIC .Antibiotics (Ampicillin, Amoxicillin) have been chosen to contrast their activity. Furthermore, Anti-fungal activity against two types of fungi ʺAspergillus flavusʺ and ʺPenicillum Spp.ʺ was studied for these compounds. The results of the antibacterial activity were better compared to the standard drugs.


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