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العنوان
Design, Synthesis, H2S release and Biological Investigation of New Hydrogen Sulfide Donors /
المؤلف
El gedamy, Arwa Mohamed Adel Awad.
هيئة الاعداد
باحث / أروى محمد عادل عوض الجدامى
مشرف / جمال الدين على أحمد حسن أبورحمه
مشرف / مي السيد مرسى شومان
مشرف / الشيماء محمد نجيب
الموضوع
Pharmacology.
تاريخ النشر
2023.
عدد الصفحات
108 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة
تاريخ الإجازة
23/1/2023
مكان الإجازة
جامعة المنيا - كلية الصيدلة - الكيمياء الطبية
الفهرس
Only 14 pages are availabe for public view

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Abstract

The present study is concerned with the design and synthesis of new amides and their corresponding potential H2S donors thioamide, sulfides and disulfides analogus of ciprofloxacin / H2S donors hybrids and biological evaluation of their antibacterial and antifungal activities. In addition, a group of thiazolidine derivatives were prepared as analogus to temonacic acid as potential H2S donors The thesis consists of four main sections: introduction, the aim of the work, results and discussion and experimental sections in addition to references and summary.
1- Introduction:
The introduction included a broad summary of the literature on the chemistry of H2S, techniques of measuring H2S, and biological activities of H2S donors. The antimicrobial fluoroquinolones, their modern derivatives, their various biological activity, and their mode of action are also covered.
2- Aim of the work:
This section outlined the goals and objectives for the design of the research,In addition to studying the mechanism of some of the synthesised compounds antibacterial, antifungal, and hepatoprotective activity, including the synthesis of the target compounds and their biological evaluation.
3- Results and discussion:
This section is subdivided into three main parts:
A-The first part (chemistry section)
It describes many processes utilized to synthesize the intermediates as well as the corresponding, final desired products. Additionally, it showed structural elucidation of these compounds using various spectroscopic techniques, including 1H-NMR, 13C-NMR spectroscopy and elemental microanalysis.
In this work synthesis of the following compounds were reported:
• fifiteenreported intermediates 2a-d, 3a-c, 10a -h
• One new intermediates 3d.
• New eight final compounds (4a-d and 6-9)
B-The second part measurement of H2S release
Methylene blue assay was used to check thirteen compounds (4a-d, 6-8 and 10a-f) for the release of H2S. All compounds released H2S, while compound 4a releasing the highest precentage H2S while other compounds only showed mild to moderate H2S.
C-The third part Biology section
This section is subdivided into two parts
i. Evaluation of the antibacterial and antifungal activities
The antibacterial and antifungal activities of compounds 3a-d, 4a-d and 6-8 were evaluated in vitro against Staphylococcus aureus, Methicillin Resistant Staphylococcus aureus, Escherichia coli and Candida albicans using ciprofloxacin as reference drug for antibacterial activity. Some derivatives displayed broad spectrum antibacterial activity as compound 4d showed the highest antiacterial activity, other derivatives showed moderate to weak activity.
i.i. Evaluation of hepatoprotective activities
Eight compounds 10a-g and compound 7 were evaluated in vivo against hepatic damage resulted from exposure to Carbon tetrachloride using l-cysteine as reference drug for hepatoprotective effect, respectively. Some derivatives displayed hepatoprotective activity as compounds 10a,10c,10e,10f and compound 7 show the highest hepatoprotective activity, while others showed moderate to weak activity.
4- Experimental section:
The specific steps taken in the various experiments are described in this section. There are five parts as following:
i- The first Part
The various processes employed to synthesis the target compounds 4a-d, 6-9 and 10a-h were discussed in the chemistry part of this chapter. The complete spectroscopic and analytical information of the produced compounds was also supplied in this section.
ii- The second part:
The methodologies used to quantify H2S release from the synthesized compounds are included in this section.
iii- The third part:
Biology section, this part outlined the method used to investigate the antibacterial and antifungal activity of the synthesized compounds 3a-d, 4a-d and 6-9 .
iii-The fourth part:
Outlined the methods used to investigate the hepatoprotective effect of the synthesized compounds 10a-g.
iii-The fifth part:
Histopathological study to investigate the hepatoprotective effect of the synthesized compounds 10a-g.