الفهرس 
IntroductionOnly 14 pages are availabe for public view
 |  | from | 159 |  |  |
| | | from | 159 | | |
Abstract
This thesis focuses on the development and synthesis of novel 1,2,4-triazole derivatives, followed by an assessment of their antimicrobial and antifungal efficacy. The thesis consists of four main sections: introduction, aim of the work, results & discussion and experimental in addition to references and Arabic summary.
1. Introduction:
The introduction provides a comprehensive summary of the synthesis of different triazole derivatives and the existing literature on antimicrobial triazoles, including new derivatives, their diverse biological effects, and the underlying mechanisms of action. Furthermore, this section represents the recent advancements in the field of chemistry and biology regarding triazoles, with particular emphasis on their unique biological uses and the crucial structural characteristics necessary for their antibacterial and antifungal properties.
2. Aim of the work:
This section outlined the goals and objectives for the design of this research including synthesis of the target compounds and biological evaluation as antibacterial and antifungal agents, in addition to studying the mechanism of antifungal activity induced by some of the synthesized compounds.
3. Results and discussion
This section is subdivided into three main parts:
A-The chemistry part:
The chemistry part provides a comprehensive account of the many methodologies employed in the synthesis of intermediates, as well as their respective end products. Furthermore, the compounds were subjected to several spectroscopic techniques such as 1H NMR, 13C NMR spectroscopy, and mass spectroscopy in order to provide structural elucidations.
In this work we reported the synthesis of the following compounds:
1. One reported intermediate 4a.
2. Two new intermediates including 4b, 4c.
3. New twenty one final compounds 6a-c , 9a-q , 10
B- Measurement of H2S release part:
Methylene blue assay was used to check one compound 10 for the release of H2S.
C-The biology part:
This section, this section is subdivided into three parts:
1. Evaluation of the antibacterial activities
The antibacterial activities of compounds 4a-c, 6a-c, 9a-q and 10 were evaluated in vitro against Staphylococcus aureus, Klebsiella pneumoniae, Escherichia coli using ciprofloxacin as reference drug for antibacterial activities. Some derivatives displayed broad spectrum antibacterial as compounds 6b, 9a, 9f and 9l. While others showed moderate to weak activity.
2. Evaluation of the antifungal activities
The antifungal activities of compounds 4a-c, 6a-c, 9a-q and 10 were evaluated in vitro against, Candida albicans and Aspergillus niger using fluconazole as reference drugs for antifungal activities. Some of the tested compounds showed remarkable antifungal activity against Aspergillus niger than that of the reference fluconazole such as compounds 6c and 9d. While others showed from good to weak or no activity. The designed compounds had no activity against Candida albicans.
3. Investigation of metal chelation as antimicrobial mechanism of target compounds
The assay was carried out according to the method of Santos and it was found that compounds 4c, 9f and 9l exert their antimicrobial action through metal chelation that consequently affect the regulatory, uptake and detoxification systems in pathogens.
4- Experimental section
This section outlines the detailed procedures of different experiments used. It includes three parts;
A- The first Part:
Chemistry section, this section described the different procedures used for synthesis of the target compounds 4a-c, 6a-c, 9a-q and 10. This section also presented all detailed spectroscopic and analytical data of the synthesized compounds.
B- The measurement of H2S release part:
The methodologies used to quantify H2S release from the synthesized compounds are included in this section
C- The biology part:
Biology section, this part outlined the method and procedures used to investigate the, antibacterial and antifungal activities of the synthesized compounds 4a-c, 6a-c, 9a-q and 10 and investigation of metal chelation as antimicrobial mechanism of target compounds 4c, 6b, 6c, 9f and 9l.