الفهرس 
Aim of the workOnly 14 pages are availabe for public view
 |  | from | 199 |  |  |
| | | from | 199 | | |
Abstract
The work in the thesis will oriented to preparation and characterization of some new
amide compounds and their metal complexes hoping to explore some effective
compounds to be used in treatment of some microbial diseases and in the treatment of
cancer. The first part of the thesis will be oriented to synthesis of some new amide
compounds resulted from the condensation of para-phenylenediamine with salicylic
acid. This product will be characterized by means of chemical analysis as well as
various spectroscopic techniques such as: elemental and thermal analyses, IR, 1H NMR,
UV-Vis, ESR, Magnetism (meff ), Mass spectroscopy , scanning and transmission
elelctron microscopy, X-ray diffraction (XRD) and some analytical techniques such as
analytical titration and fluorescence spectroscopy. Finally, The biological study ,
antimicrobial activities of the prepared ligand and its metal complexes against grampositive
bacterium (Staphylococcus aureus and Bacillus subtilis), gram negative
bacterium (Escherichia coli and Pseudomonas aeruginosa) and Fungus (Candida
albican) and studying the cytotoxicity and cell viability against some of human
cancerous cell line ; prostate cancer cell line (PCL-3), in-vitro screening was done.
The work consisted of three main parts
I- Introduction
This chapter includes an overview of previous research for amide ester
compounds, general methods of preparation, properties, importance and their
applications. The general methods of preparation of amides were depeded on some
usual methods such as substitution reactions. Recently, the electrosynthesis of amids
was the perfect method of preparation. Amide and their derivatives constitute a versatile
class of compounds in organic chemistry. These compounds associated with broad
spectrum of biological activities. Literature survey reveals that nitrogen - and sulfurcontaining
compounds showed very good bioactivity, including antituberculosis,
anticonvulsant, analgesic antiinflammatory, insecticidal, antifungal and antitumor
properties. Morpholine derivatives find their wide spectrum of antimicrobial activity
B
Summary
and exhibit anthelmintic, bactericidal and insecticidal activity. They are also involved as
an intermediate product in the synthesis of therapeutic agents. Amide derivatives also
show anti-platelet activity. Bioactivity of amides can also be achieved by constructing
the amide with hydroxypentanedioate.
Nanotechnology offers great visions of improved, personalized treatment of disease.
The hope is that personalized medicine will make it possible to develop and administer
the appropriate drug, at the appropriate dose, at the appropriate time to the appropriate
patient. The benefits of this approach are accuracy, efficacy, safety and speed. Today,
commercial nanomedicine is at a nascent stage of development and it’s full potential
years or decades away. Currently, the most advanced area of nanomedicine is the
development and use of nanoparticles for drug delivery
II- Experimental
This chapter contains the chemical and instruments used in practical part of the
thesis as follow:
1) Preparation of amide ester ligand and its metal complexes.
2) characterization of the ligand and its complexes using:
Physical techniques such as molar conductance, magnetic susceptibility and
melting point.
Elemental analyses (C, H, N, Cl and M).
Spectral techniques as IR, UV- Vis., 1HNMR, mass spectra and ESR
measurements.
Thermal techniques as DTA and TGA
Measuring the particleʼs diameters using transmission electron microscope
3) Measurement of Antibiological activity. antimicrobial activities of the prepared
ligand and its metal complexes against gram-positive bacteria (Staphylococcus
aureus and Bacillus subtilis), gram negative bacteria (Escherichia coli and
Pseudomonas aeruginosa) and Fungus (Candida albican) and also studying the
cytotoxicity and cell viability against prostate cancer cell line (PCL-3).
C
Summary
III- Results and discussion
This chapter includes characterization of the ligand and its metal complexes. The
ligand was prepared by esterification reaction between salicylic acid and ethanol by
adding five drops of conc H2SO4. The mixture was refluxed on water bath for 1 hour
with para-phenylenediamine and then left to cool at room temperature and then was
stirred for 30 minutes. After cooling, the solvent was removed under reduced pressure
to give crude product which was crystallized in ethanol to yield pure ligand (1). The
yield of the ligand was 83 % with m.p. 296 and black color. The metal complexes (2 –
15) were prepared by refluxing with string a suitable amount of a hot ethanolic
solution of the ligand with different metal salts.
All the metal complexes are stable at room temperature, insoluble in water, not
hydroscopic , partially soluble in MeOH, EtOH, CHCl3 and (CH3)2CO and completely
soluble in DMF and DMSO. These complexes have been characterized by some
instumental analysis methods such as 1H-NMR, mass, IR, UV-VIS, ESR spectra,
magnetic moments and conductance measurements, elemental and thermal analyses.
Furthermore, the ligand HL (1), Cu(II) complex (6), Zn(II) complex (11) and Ag(I)
complex (12) exhibit fluorescent properties; the proposed spectrofluorimetric method is
simple, accurate, sensitive.
Cytotoxic evaluation of the complexes as antimicrobial has been carried out.
Complexes show enhanced activity in comparison to the standard drug used. These
organometallic complexes candidates as antimicrobial agents. against two bacterial
strains; Gram-positive Staphylococcus aureus as well as Gram-negative Escherichia
coli strains. The complexes were also subjected to antifungal activity against Candida
albicans.
The anti-tumor activity against prostatic carcinoma cell line of the ligand and its
complexes have been carried out. Ligand (1) and its complexes showed enhanced
activity in comparison to the standard drug (Cisplatin) was applied with IC50 = 8.51-
D
Summary
401.18 μg/ml range. Zn(II) complex (11) was the most potent cytotoxic agent against
prostatic carcinoma with IC50 = 8.51 μg/ml which candidates as anticancer agent.
from all above, the ligand HL (1) and some of its metal complexes can be used as
anti-tumor, antibacterial and antifungal agents by compareson with the standard
commercial drugs.