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العنوان
Prospective biologically novel heterocycles from reactions of amidrazones /
المؤلف
Fathy, Hazem Mohamed.
هيئة الاعداد
باحث / حازم محمد فتحي
مشرف / أشرف عبدالمنعم علي
مشرف / محمد عبدالعزيز محمد عثمان
مشرف / محمد رمضان عيسي
الموضوع
Pharmacy. Pharmaceutical chemistry.
تاريخ النشر
2016.
عدد الصفحات
171 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة
تاريخ الإجازة
1/1/2016
مكان الإجازة
جامعة المنيا - كلية الصيدلة - قسم الكيمياء الطبية
الفهرس
Only 14 pages are availabe for public view

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Abstract

The thesis is divided into five sections:
Introduction
Include an overview of the different methods that were used in the synthesis of amidrazones and their derivatives using different means and also included provided on the study of the use of Amidrazones in the synthesis of many compounds heterocyclic compounds like pyrazoles , triazoles, thiadiazoles, and pyrimidinones. Also included provided on biological activities of Amidrazones like anti-biotic, anti-parasitic, antifungal and anti-cancer. Also as antimalarial, radiotherapy, analgesic and anti-inflammatory. Also amidrazones used to decrease skin damage. Amidrazones when form complexes with vanadium showing insulin-mimetic activity. Amidrazones improve insulin sensitivity and promote weight loss. Amidrazones used in synthesis of pyrazoles which used antidepressant, anti-influenza, anticancer, antiaggregating, anti-biotics, anti-histaminic, antioxidant and anticonvulsant.
Field of thesis
Includes target conducted study for it as well as the aim of work such as synthesis of pyrazoles and pyrimidinones through reaction of amidrazones as an example of electron donors with compounds of the type  as an example of electron acceptor.Study of their effectiveness as antagonist of TRP, anti-inflammatory and anti-cancer.
Results and discussion
Chemistry part includes discussion of results of the synthesis of target compounds and make sure the structure by using differnet spectroscopic techniques such as IR, NMR, mass spectroscopy and X-ray. Biological studies part which reveal the results of biological studies and includes measuring the effectiveness of some final compounds as antagonist of TRP which play roles in sensory physiology, sensing the outside world so contribute in vision, taste, olfaction, hearing, touch, sensing local cellular environment, secretion of fluids and hormones, kidney, urinary bladder, and bone function. In addition, mutations in genes encoding TRP channels are the cause of several inherited diseases that affect a variety of systems including the renal, urinary bladder, skeletal and nervous system. Increasing number of gene deletion studies in animals and genetic association studies in humans have demonstrated that the pathophysiological roles of TRP channels, which include (but are not limited to) respiratory reflex hypersensitivity, cardiac hyper¬trophy, renal disease. The results showed there are one compounde revealed anti-TRP by inhibition of prey capture in hydra plant. Also the Screening of anti-inflammatory activity by inhibition of COX-2 enzyme which convert arachidonic acid to prostaglandine which play important role in inflammatory action. Also the biological activities of pyrazoles as anti-cancer which confirmed by using MTT assay in human embryonic kidney cells (colourimetric method) and the results revealed there are two compounds showed anti-cancer activity by inhibition of cell viability and to understand the mechanism of anti-cancer activity we used western blott methods by using two different proteins, the first is the proliferating cell nuclear antigen (PCNA) and the second is the murin double minute 2 protein (MDM2). The results revealed there are five compounds succeded to inhibit MDM2 and there are two compounds succeded to inhibit PCNA.
Experimental
Includes detailed explantation of all experiments as well as detailed analysis of all final compounds
References
Includes of 153 references between the old and recent references until 2016 and this part in 12 papers.