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Synthesis of some Novel Nitrogenous Heterocyclic Compounds with Expected Biological Activity as Antimicrobial and Cytotoxic Agents
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This study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential  activity as antimicrobial and/or cytotoxic.  Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.

These pharmacological properties of quinolones  aroused our  interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linked to amino acid ester or heterocyclic amine with the aim of obtaining a pharmacologically active compounds.O-alkylation has been done on( 8-hydroxyquinoline ) to get (O-alkylated ester) derivatives which are deesterfied to get acetic acid derivatives, then coupled with amino acid that have protected carboxyl group (amino acid esters) or heterocyclic amine by using conventional solution  method for peptide synthesis as a coupling method.

The proposed analogues were successfully synthesized and the processing of the reactions confirmed by TLC ,the synthesized  analogues with the proposed structures as they were characterized and proved by  melting point, infrared spectroscopy (IR) and elemental microanalysis.

The tested analogues showed cytotoxic activity on the HEp-2 cell line (tumor of larynx) with inhibitory concentration percent of (IC %) range (32.43 % - 49.55%) and showed that the tested compounds had variable antimicrobial activities against selected bacteria and yeast when compared with selected standard drugs.

Keywords: Quinolones, 8-hydroxyquinoline , N-heterocycles biological activity.

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Publication Date
Sat Jun 01 2024
Journal Name
Minar International Journal Of Applied Sciences And Technology
PREPARATION, CHARACTERIZATION AND EVALUATE THEIR BIOLOGICAL ACTIVITY OF NEW HETEROCYCLIC COMPOUNDS DERIVED FROM 4-((1-(4-HYDROXYPHENYL) ETHYLIDENE) AMINO) BENZENESULFONAMIDE
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The research included the preparation of cyclic compounds from thiazoles, imidazoles and oxazepines from the reaction of cyclization starting material that acts Schiff bases, which is a raw material in the formation of cyclic compounds from Schiff's(B1) by reaction of 4- aminobenzenesulfonylamide with 4-hydroxyacetophenone which can used to synthesized two lines. The first introducing the preparation of pyrazoles [B4, B5] from ester [B2], which derived to acid hydrazide[B3] with hydrazine hydrate and final pyrazoles obtained by the reaction with diethylmalonate and acetylacetone. The second including prepared the new 1,3-oxazepine1,5-dione derivatives[B6,B7,B8] from adding different anhydrides to the base[B1] as a seven membered ring ; te

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Publication Date
Thu Feb 28 2019
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis of some Schiff base metal complexes involving trimethoprim and 2'-amino-4-chlorobenzophenone: Spectral, thermal, DNA Cleavage antimicrobial,antifungal and Cytotoxic activity studies
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In study of effective bioactive compounds, we have synthesized the Co((ІІ), Mn(ІІ), Fe(ІІ), Cu(ІІ), Ni(ІІ), and Zn(ІІ) complexes of the Schiff base derived from trimethoprim and2'-amino-4-chlorobenzophenone and characterized by spectroscopic (NMR, IR, Mass, UV–vis,), analytical, TGA studies and magnetic data .The solution electronic spectral study suggests the stoichiometry of the synthesized complexes and Elemental analysis detected the square planer and octahedral geometry of the compounds. The prepared metal complexes presented promoted efficiency versus the screened bacterial (Escherichia Coli and Staphylococcus aureus) antibacterial efficacy against (Staphylococcus aureus, Salmonella spp., E. coli, Vibrio spp., Pseudomona

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Publication Date
Fri Feb 01 2019
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis of some Schiff base metal complexes involving trimethoprim and 2'-amino-4-chlorobenzophenone: Spectral, thermal, DNA Cleavage antimicrobial,antifungal and Cytotoxic activity studies
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In study of effective bioactive compounds, we have synthesized the Co((ІІ), Mn(ІІ), Fe(ІІ), Cu(ІІ), Ni(ІІ), and Zn(ІІ) complexes of the Schiff base derived from trimethoprim and2'-amino-4-chlorobenzophenone and characterized by spectroscopic (NMR, IR, Mass, UV–vis,), analytical, TGA studies and magnetic data .The solution electronic spectral study suggests the stoichiometry of the synthesized complexes and Elemental analysis detected the square planer and octahedral geometry of the compounds. The prepared metal complexes presented promoted efficiency versus the screened bacterial (Escherichia Coli and Staphylococcus aureus) antibacterial efficacy against (Staphylococcus aureus, Salmonella spp., E. coli, Vibrio spp., Pseud

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Publication Date
Sun Nov 13 2022
Journal Name
Journal Of Kufa For Chemical Sciences
Preparation, characterisation and biological activity of some metal complexes derived from new dithiocarbamate of heterocyclic ligand
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In this study, synthesised new ligand: potassium 2,2'-(quinoxaline-2,3- diyl)bis(1-phenylhydrazinecarbodithioate) (L). The ligand synthesised by reacting N1,N2-dip-tolyloxalamide as the starting material with CS2 and KOH to add the CS2 group and then with phenylendiammine to achieve (L). The ligand used in the synthesis of complexes with (CoII, NiII and CdII). The new ligand and its complexes characterised by FT-IR, UV-Vis, 1H, 13C-NMR, Mass spectroscopy, and elemental analysis, in addition to the above techniques were using magnetic moment, atomic absorption, chloride content, and melting point to describe the metal complexes.

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Publication Date
Thu Feb 01 2024
Journal Name
Doklady Chemistry
Synthesis, Characterization, and Biological Evaluation of New Cyclic Quinazoline Derivatives as Potential Antibacterial and Antifungal Agents
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Heterocyclic compounds are crucial for medicinal chemistry and the development of therapeutic agents like broad-spectrum antibiotics. This study devised a facile procedure to synthesize novel antimicrobial bicyclic heterocycles from 2-mercapto-3-phenylquinazolin-4(3H)-one. Advanced analytical techniques including 1 H and 13C NMR, elemental analysis, and FT-IR spectroscopy characterized the intricate chemical structures of the products. In vitro assays tested the heterocycles against aerobic and anaerobic bacterial strains using fluconazole and ciprofloxacin as antifungal and antibacterial controls. Results demonstrated the formidable broad-spectrum antibacterial and antifungal activities of the synthesized compounds, with growth inhibition

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyrazoline and Isoxazoline Derivatives as Antibacterial Agents
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In this paper some chalcones (C1-C8) are prepared based on the reaction of one mole of substituted acetophenone with one mole of substituted benzaldehydes in the presence of (40%) sodium hydroxide as a base. Pyrazolines (P1–P8) are prepared from the reaction of chalcones (C1-C8) with hydrazine hydrate. Isoxazoline (I1-I8) is prepared from the reaction of chalcones (C1-C8) with hydroxyl amine hydrochloride in the presence of (10%) sodium hydroxide as a base. These compounds are characterized by using various physical and spectral methods. The compounds are screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria. Several derivatives of pyrazolines and isoxazolines are produced well to moder

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Publication Date
Sat Nov 05 2022
Journal Name
Hiv Nursing
Coordination Compounds of Carbonyl Oxygen and Indole Nitrogen Bidentate Ligand; Synthesis, Structural Characterisation and Biological Activity
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The synthesis of the bisaldehyde ligand 2-(1,1-dimethyl-1,3-dihydro-2H-benzo[e]indol-2-ylidene)malonaldehyde (B) and its coordinated compounds with Cr(III), Mn(II), Fe(II), Co(II), Ni(II) and Cu(II) ions are reported. The synthetic route of B was completed by adopting the Vilsmeier-Haack reaction. This was based on the mixing of 1,1,2-trimethyl-1H-benzo[e]indole with phosphoryl trichloride and N, N-dimethylformamide (anhydrous) that gave the aminomethylenemalondialdehyde. The use of POCl3 and DMF was aimed to give the Vilsmeier-Haack intermediate, which was kept at 5°C and then heated with stirring at 85°C. The addition of an aqueous NaOH solution (35%) to the reaction mixture resulted in the isolation of B. The monomeric coordinated comp

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Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
First Transition Metal Complexes Salts of Diazonium Derived from Nitrogen Heterocyclic Compound, Synthesis, Characterization and Biological Activity
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Metal complexes chrome(III), manganese(II), iron(III), cobalt(II), nickel(II), cupper(II) and zinc(II) with diazonium of 3-amino-2-chloropyridine of general formula [2-Cl-C5H3N≡N]n[MXm], where n=2 or 3 for divalent and trivalent metal, m= 4 or 6  were synthesized. The complexes have been characterized by flame atomic absorption, (C.H.N), molar conductance, magnetic susceptibility UV-vis spectra, infrared spectra,1H-NMR spectroscopy and thermo gravimetric analysis (TGA and DTA). The measurements showed that the divalent metal ion complexes (M2+) have (1:2) M:L ratio with tetrahedral geometry around metal ions while the trivalent metal ions (M3+) formed (1:3) m

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Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
Synthesis of gamma biguanides butyric acid analogues as HDAC inhibitors and studying their cytotoxic activity
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Publication Date
Sun Dec 30 2018
Journal Name
Baghdad Science Journal
Synthesis and study of biological activity of some new Imidazole derivatives
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In this work ester derivatives were synthesized by the reaction of imidazole derivatives (C1) with ethylchloroacetate in ethanol and NaOH to give the corresponding (C2) .While compound (C3) acetohydrazide was synthesized by the reaction of ester derivatives (C2) with hydrazine hydrat in ethanol. Compound (C3) from the reaction with different aromatic aldehydes in absolute ethanol gave the Schiff′s bases (C4,C5). The product compounds were characterized by FT-IR, U.V and 1HNMR spectra and the biological activities were studied as antibacterial.

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