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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
Sun May 10 2020
Journal Name
Baghdad Science Journal
Characterization and Biological Activity of Some New Derivatives Derived from Sulfamethoxazole Compound: new derivatives from sulfamethoxazole drug.
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 A new series of Sulfamethoxazole derivatives was prepared and examined for antifibrinolytic and antimicrobial activities. Sulfamethoxazole derivatives bear heterocyclic moieties such as 1,3,4-thiadiazine {3},  pyrazolidine-3,5-diol {4} 6-hydroxy-1,3,4-thiadiazinane-2-thione {5} and [(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)diazenyl] {8}. Their structures were elucidated by spectral methods (FT-IR, H1-NMR). Physical properties are also determined for all compound derivatives.  Recently prepared compounds were tested for their antimicrobial activity in the laboratory. Each screened compound showed good tendency to moderate antimicrobial activity.

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Publication Date
Thu Dec 01 2022
Journal Name
Environmental Nanotechnology, Monitoring & Management
Synthesis of nano-magnetite and magnetite/synthetic geopolymer nano-porous composite for application as a novel adsorbent
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In this work magnetite/geopolymer composite (MGP) were synthesized using a chemical co-precipitation technique. The synthesized materials were characterized using several techniques such as: “X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), vibrating sample-magnetometer (VSM), field-emission scanning electron microscopy (FE-SEM), energy dispersive X-ray spectroscopy (EDS), Brunauer–Emmett–Teller (BET) and Barrentt-Joyner-Halenda (BJH)” to determine the structure and morphology of the obtained material. The analysis indicated that metal oxide predominantly appeared at the shape of the spinel structure of magnetite, and that the presence of nano-magnetite had a substantial impact on the surface area and pore st

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Publication Date
Wed Nov 01 2023
Journal Name
Journal Of Dentistry
The in-vitro development of novel enzyme-based chemo-mechanical caries removal agents
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Objectives Bromelain is a potent proteolytic enzyme that has a unique functionality makes it valuable for various therapeutic purposes. This study aimed to develop three novel formulations based on bromelain to be used as chemomechanical caries removal agents. Methods The novel agents were prepared using different concentrations of bromelain (10–40 wt. %), with and without 0.1–0.3 wt. % chloramine T or 0.5–1.5 wt. % chlorhexidine (CHX). Based on the enzymatic activity test, three formulations were selected; 30 % bromelain (F1), 30 % bromelain-0.1 % chloramine (F2) and 30 % bromelain-1.5 % CHX (F3). The assessments included molecular docking, Fourier-transform infrared spectroscopy (FTIR), viscosity and pH measurements. The efficiency

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Publication Date
Wed Nov 01 2023
Journal Name
Journal Of Dentistry
The in-vitro development of novel enzyme-based chemo-mechanical caries removal agents
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Objectives: Bromelain is a potent proteolytic enzyme that has a unique functionality makes it valuable for various therapeutic purposes. This study aimed to develop three novel formulations based on bromelain to be used as chemomechanical caries removal agents. Methods: The novel agents were prepared using different concentrations of bromelain (10–40 wt. %), with and without 0.1–0.3 wt. % chloramine T or 0.5–1.5 wt. % chlorhexidine (CHX). Based on the enzymatic activity test, three formulations were selected; 30 % bromelain (F1), 30 % bromelain-0.1 % chloramine (F2) and 30 % bromelain-1.5 % CHX (F3). The assessments included molecular docking, Fourier-transform infrared spectroscopy (FTIR), viscosity and pH measurements. The efficie

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Publication Date
Thu May 10 2018
Journal Name
Global Journal Of Health Science; Issn 1916-9736 E-issn 1916-9744
Effects of Biological and Non Biological Agents (Disease Modifying Antirheumatic Drugs) on Bone Mineral Density in a Sample of Rheumatoid Arthritis Patients
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Background: Osteoporosis is an extra-articular complication of rheumatoid arthritis that results in increased risk of fractures and associated morbidity, mortality, and healthcare costs. Objective: To evaluate changes in bone mineral density in a sample of rheumatoid arthritis (RA) patients on biological (anti tumor necrosis factor (TNF) alpha) and non-biological agent disease modifying antirheumatic drugs (DMARDs). Patients and Methods: A cross sectional study enrolled 60 RA patients diagnosed by rheumatologist according to the 2010 American College of Rheumatology/European League Against Rheumatism (2010 ACR/EULAR) classification criteria for RA. Thirty patient on biological agent (anti TNF alpha) and 30 patient on non-biological agent (D

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Publication Date
Fri Sep 01 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Studying the Enzyme Activity of New Benzothiazole Schiff Base Ligand (HL) and Its Complexes with Some of Metal Ions
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Publication Date
Sun Dec 24 2023
Journal Name
Journal Of The College Of Basic Education
Structural, Characterization, Biological and Studying the Enzyme Activity of some transition metal complexes with 4- )(2- hydroxy phenyl imino) methyl) -2, 6-dimethoxy phenol
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A new Schiff bases ligand 4- ((2-hyolroxy phenylimino) methyl) -2, 6-dimethoxyphenol  derived from condensation of 2- amino phenol with 4-hydroxy -3, 5-dimethoxy benzaldehyde have been synthesized and characterized by  spectroscopy,  spectra, Mass spectrum and elemental microanalysis (C.H.N). Metal Complexes with ions have been also synthesized and characterized spectroscopic methods  spectroscopy, flame atomic absorption, molar conductivity measurements and magnetic susceptibility. These studies indicate that the moler ratio  for the complexes. The complexes  showed characteristics octahedral geometry with the (O,N) ligand coordinated in bidentate mode while with  showed square planer. The enzyme activity of the ligand and i

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Publication Date
Mon May 30 2022
Journal Name
Egyptian Journal Of Chemistry
Design ,Synthesis, Insilco Study and Biological Evaluation of New Coumarin-Oxadiazole Derivatives as Potent Histone Deacetylase Inhibitors
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Publication Date
Thu Oct 01 2020
Journal Name
Biochem. Cell. Arch
NEW ORGANOTIN(IV) COMPLEXES DERIVED FROM 3,4-DIHYDROXYBENZALDEHYDEN(4)-ETHYL-3-SEMICARBAZONE LIGAND: SYNTHESIS, CHARACTERISATION AND BIOLOGICAL ACTIVITY
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Two new organotin(IV) complexes Me2Snesc (C1) and Bu2Snesc (C2) have been synthesised from the reaction of the corresponding organotin(IV) chloride with the Schiff base ligand 3,4-dihydroxybenzaldehyde-4-ethylsemicarbazone (H2esc). The ligand was prepared in two steps. The first step includes the formation of 4-ethylsemicarbazide, which then reacted with 3,4-dihydroxybenzaldehyde to give the title ligand. Complex formation between the organotin(IV) moiety and the anionic form of 3,4-dihydroxybenzaldehy-4-ethylsemicarbazone occurred through the o-dihydroxy positions. The ligand and its complexes were characterised by elemental analysis, FT-IR and NMR (1H, 13C and 119Sn) spectroscopy. Accordingly, the complexes were proposed to have tetrahedr

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Publication Date
Sat Dec 15 2018
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis, Spectroscopic and Antimicrobial Studies of Mixed Ligand Metal (II) Complexes with three amino acids
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The research includes synthesis and identification of novel three amino acids ligands complexes of some heavy metal (II) ions by using the amino acids like glycine, L-alanine and L-valine. New metal mixed ligand complexes with amino acids are prepared the reaction by reacting the three amino acids with the metals(II) chloride by using 50% ethanolic solution and 50% distall water in the molar ratio [1:1:1:1] ( M:Gly:Ala:Val) except for Co(II) and Ni(II) complexes were found after diagnosis the coordination with both Lalanine and L-valine. The prepared complexes identified by using physical properties, flame atomic absorption and conductivity measurements, in addition, mass, FT.IR and UV.vis spectrum as well magnetic moment data. The general

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