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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
Tue Dec 16 2014
Journal Name
Iraqi National Journal Of Chemistry
Synthesis of Novel Heterocyclic Compounds via Schiff bases
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In the present study a series of some four-,five-and seven-membered heterocyclic compounds have been synthesized by the reaetion of Schiff bases (1a,b) with chloroacetyl chloride, sodium azide, thioglycolic acid or various anhydrides to give azetidinone (2a,b), tetrazole (3a,b), thiazolidinone (4a,b) and 1,3-oxazepine derivatives (5-8a,b) respectively. Schiff bases (1a,b)were prepared from the reaction of p-toluidine with aromatic aldehydes. All synthesized compounds were characterized by physical properties and spectral data.

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Publication Date
Sun Sep 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Evaluation of Antimicrobial Activity of Few New Heterocyclic Compounds Derived from Nicotinic Acid
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New schiff bases series (VIII) a-e and 1,3-thiazolidin-4-one derivatives (IX) a-e containing the 1,2,4-triazole and 1,3,4-thiazazole rings were synthesized and screening their biological activities. These compounds were identified via Fourier transform infrared (FT-IR) spectra, some via Proton nuclear magnetic resonance (1H-NMR) and mass spectra. The biological results indicated that all of these compounds did not reveal antibacterial effectiveness against (Escherichia coli and Klebsiella species) (G-). Some of these compounds showed moderate antibacterial activity against (Staphylococcus aureus, and Staphylococcus epidermidis) (G+), and all compounds exhibited moderate activity against Candida albicans.

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Scopus (1)
Scopus
Publication Date
Thu Aug 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis, Characterization of Different Five-Membered Heterocyclic Derivatives, Evaluated Their as Antioxidant, and In Vitro Antimicrobial Agents
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Objective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid,

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Publication Date
Sun Mar 08 2020
Journal Name
Biochem. Cell. Arch
SYNTHESIS AND SPECTROSCOPIC CHARACTERIZATION OF NEW HETEROCYCLIC COMPOUNDS DERIVATIED FROM 1-(4-AMINOPHENYL) ETHAN-1-ONEOXIME AS A STARTING MATERIAL WITH EVALUATE THEIR BIOLOGICAL ACTIVITY
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ABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis of some Heterocyclic Compounds Derived from
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The 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending u

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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)
Preliminary Cytotoxic Study of Some Novel Furo-2-quinolone Compounds
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In this research, new series of Furo-2-quinolone [FQ] compounds have been synthesized. These novel [FQ] compounds were prepared from coumarin derivatives (Furocoumarins: psoralen and isopsoralen).Identifications of these FQ compounds were performed by using infrared spectrum (I.R), Ultraviolet spectrum (U.V) and Nuclear Magnetic Resonance spectrum (H1-NMR) besides some physical data. The cytotoxic screening involves ;using HEP-2 cell line which gave differential responses against tested compounds : 4,6 Dimethyl furo[2, 3-g] coumarin (C1), 1-(2`, 4`, Dimethoxy benzylideneimino)-2,6-dimethyl Furo [2, 3-g] quinoline-2-one (C3) and the angular psoralen of the same derivative

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Crossref (1)
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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and characterization of some heterocyclic including oxazoles,Thiazoles, Pyridazines, phthalizines and Pyrazoles with evaluating of biological activity.
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A series of new compounds including p-bromo methyl pheno acetate [2]. N-( aminocarbonyl)–p-bromo pheno acetamide [3] , N-( aminothioyl) -p-bromo phenoacetyl amide [4], N-[4-(p-di phenyl)-1,3-oxazol-2-yl]-p-bromopheno acetamide [5],N-[4-p-di phenyl]-1,3-thiazol-2-yl-p-bromo phenoacet amide [6], p-bromopheno acetic acid hydrazide [7] , 1-N-(p-bromo pheno acetyl)-1,2-dihydro-pyridazin-3,6- dione [8], 1-N-(p-bromo pheno acetyl)-1,2-dihydro-phthalazin-3,8- dione[ 9], 1-(p-bromo pheno acetyl)-3-methylpyrazol-5-one [10] and 1-(p-bromo phenol acetyl)- 3,5-dimethyl pyrazole [11] have been synthesized. The prepared compounds were characterized by m.p.,FT-IR and 1H-NMR spectroscopy. Also ,the biological activity was evaluated .

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Publication Date
Sat Dec 01 2012
Journal Name
Asian Journal Of Chemistry
Microwave assisted synthesis of new heterocyclic compounds: 1, 2, 3-triazoles and tetrazoles and study of their biological activity
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The work includes synthesis of 1,2,3-triazoles via click conditions and using the microwave irradiation starting from two synthesized azides: 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl azide (5) and perfluorobutylethyl azide (10) and different terminal alkynes. It also includes microwave enhanced synthesis of tetrazoles via the reaction of two synthesized azides i.e., perfluorobutylethyl azide (10) and 1,5-diazidopentane (13) with benzoyl cyanide. Most of the prepared compounds have been characterized by: TLC, FT-IR, 1H NMR, 13C NMR, LC-MS and microelemental analysis

Publication Date
Wed Jan 01 2020
Journal Name
Systematic Reviews In Pharmacy
Synthesis of New Ibuprofen Derivatives Containing (Oxothiazolidin-3-yl) Amino Moiety with Expected Biological Activity
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Nonsteroidal anti-inflammatory drugs (NSAIDs) are drugs that help reduce inflammation, which often helps to relieve pain. In this research new ibuprofen oxothiazolidnone derivatives were synthesized from the reaction of Schiff base derivatives of Ibuprofen with mercapto acetic acid VI a-c, to improve the potency and to decrease the drug's potential side effects, a new series of 4-thiazolidinone derivatives of ibuprofen was synthesized VI a-c . The characterizations of the compounds were identified by using FTIR, 1HNMR technique and by measuring the physical properties.

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Scopus (3)
Scopus
Publication Date
Mon Mar 01 2010
Journal Name
Journal Of Kerbala University
Synthesis And Biological Activity Of Some New Compounds Containing 1,2,4-Triazole And Their Derivatives
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Condensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-

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