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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
Mon Jan 01 2024
Journal Name
Baghdad Science Journal
Study of the Anticancer and Antimicrobial Biological Activity of a New Series of Thiohydantoin Derivatives
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        Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The da

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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
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The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

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Publication Date
Tue Dec 30 2025
Journal Name
Iraqi Journal Of Science
Blending a New Polymers Containing Oxadiazole Ring with PVA: Synthesis , Thermal Analysis and Biological Activity
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This study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s

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Publication Date
Tue Dec 30 2025
Journal Name
Iraqi Journal Of Science
Blending a New Polymers Containing Oxadiazole Ring with PVA: Synthesis , Thermal Analysis and Biological Activity
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This study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s

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Publication Date
Sun Jan 01 2023
Journal Name
The Egyptian Journal Of Hospital Medicine
The Antimicrobial Activity of Melanin-Mediated Synthesis of Silver Nanoparticles
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Background: Nowadays, the environmentally friendly procedures must be developed to avoid using harmful compounds in synthesis methods. Their increase interest in creating and researching silver nanoparticles (AgNPs) because of their numerous applications in many fields especially medical fields such as burn, wound healing, dental and bone implants, antibacterial, viral, fungal, and arthropodal activities. Biosynthesis of nanoparticles mediated pigments have been widely used as antimicrobial agent against microorganisms. Silver nanoparticles had synthesized by using melanin from locally isolate Pseudomonas aeruginosa, and used as antimicrobial activity against pathogenic microorganisms. Aim of the study: Isolation of Pseudomonas aeruginosa

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Crossref (2)
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Publication Date
Tue Jul 09 2019
Journal Name
Journal Of Global Pharma Technology
Ni (II) and Cd (II) Complexes Derivatives from Heterocyclic Schiff Base; Synthesis, Spectroscopic and Biological Studies
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Ni and Cd complexes of new Schiff base derived from 5-Amino-2-phenyl-2,4-dihydro-pyrazol-3-one with 4-chlorobenzalaldehyde (A) , 2-Hydroxy-benzalaldehyde (B) and 4-Hydroxy-benzaldehyde (C) have been prepared and characterized by elemental analysis , molar conductivity measurements , FTIR , UV- vis , 1HNMR, mass spectrometer and magnetic susceptibility. Analytical data revealed that six complexes were a distorted tetrahedral geometry and exhibited (1:1) metal :ligand ratio. The biological activity for the three ligands and its complexes were studied

Publication Date
Thu May 15 2025
Journal Name
Chemchemtech
SYNTHESIS, CHARACTERIZATION AND SCREENING OF ANTIMICROBIAL ACTIVITY FOR SOME NEW SCHIFF BASES AND THIAZOLIDINONE DERIVATIVES DERIVED FROM AROMATIC CARBOXYLIC ACID
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In this study, the antimicrobial properties of newly synthesized Schiff bases (4a-4e) and thiazolidinone compounds (5a-5e) generated from 3,5-dinitrobenzoic acid were assessed. These compounds were obtained by reacting 3,5-dinitrobenzoic acid (1) with ethanol in a few drops of concentrated H2SO4 to produce the ester (2). The acid hydrazide (3), which was produced by treating the ester with hydrazine hydrate, reacted with the proper aldehydes, including 4-bromobenzaldehyde, 4-chlorobenzaldehyde, 4-hydroxybenzaldehyde, 4-methoxybenzaldehyde, and 4-hydroxy-3-methoxybenzaldehyde, respectively, to form Schiff bases (4a-4e). The thiazolidinone compounds (5a-5e) were produced by the cyclocondensation reaction of compounds (4a-4e) with thio

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Publication Date
Thu May 15 2025
Journal Name
Chemchemtech
SYNTHESIS, CHARACTERIZATION AND SCREENING OF ANTIMICROBIAL ACTIVITY FOR SOME NEW SCHIFF BASES AND THIAZOLIDINONE DERIVATIVES DERIVED FROM AROMATIC CARBOXYLIC ACID
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In this study, the antimicrobial properties of newly synthesized Schiff bases (4a-4e) and thiazolidinone compounds (5a-5e) generated from 3,5-dinitrobenzoic acid were assessed. These compounds were obtained by reacting 3,5-dinitrobenzoic acid (1) with ethanol in a few drops of concentrated H2SO4 to produce the ester (2). The acid hydrazide (3), which was produced by treating the ester with hydrazine hydrate, reacted with the proper aldehydes, including 4-bromobenzaldehyde, 4-chlorobenzaldehyde, 4-hydroxybenzaldehyde, 4-methoxybenzaldehyde, and 4-hydroxy-3-methoxybenzaldehyde, respectively, to form Schiff bases (4a-4e). The thiazolidinone compounds (5a-5e) were produced by the cyclocondensation reaction of compounds (4a-4e) with thio

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Publication Date
Tue Oct 20 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Biological Activity of Complexes of Some Amino Acid
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Biological Activity of Complexes of Some Amino Acid

Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
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 heati

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