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تحضير بعض مركبات الايزوكسازول - 5 - والبايرازول -5- اون المعوضة وتقييم فعاليتها البايولوجية والأنزيمية

المؤلف الرئيسي: على، ثائر عبدالله (مؤلف)
مؤلفين آخرين: خضير، خضير عباس (مشرف) , حمد، عبدالمجيد صالح (مشرف)
التاريخ الميلادي: 2011
موقع: تكريت
التاريخ الهجري: 1432
الصفحات: 1 - 115
رقم MD: 613780
نوع المحتوى: رسائل جامعية
اللغة: العربية
الدرجة العلمية: رسالة دكتوراه
الجامعة: جامعة تكريت
الكلية: كلية التربية
الدولة: العراق
قواعد المعلومات: Dissertations
مواضيع:
رابط المحتوى:

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المستخلص: The abstract of this thesis can be summarized as follows: Part 1: Organic synthesis 1- The derivatives of Isoxazolone have been synthesized from reaction of ethyl acetoacetate with Sodium metal in the presence of ether to obtain the carbanion then addition of 2,4_dinitroclorobenzen as a substituent to obtain (2,4_dinitro Aryl Acetoacetate).Using Hydroxyl amine hydrochloride the cyclisation has been achieved to obtain the isoxazolone derivative 4_(2,4_dinitro Aryl)3_methyl isoxazol_5_one. By the same method, Bromo cyclohexan was added to the carbanion to obtain (ethyl cyclohexan acetoacetate) and the cyclisation by Hydroxyl amine hydrochloride to obtain the second derivative of Isoxazolone (4_cyclohexan_3_methyl Isoxazol_5_one). Using two moles from each of these derivatives with one mole from various aldehydes and ketones afforded the bimolecular of Isoxazolone derivatives. 2- The derivatives of Pyrazolone have been synthesized using the same method except that the Hydrazine hydrate was used in the cyclisation to obtain 4_(2,4_dinitro Aryl)_3_methyl Pyrazol_5_one and 4_cyclohexan_3_methyl Pyrazol_5_one. The reaction of Pyrazolone derivatives with various Aldehydes and Ketones afforded the Dimers. 3- (2,4_dinitro Aryl acetoacetate) was closed using 2,4_dinitrophenyl Hydrazine to obtain 1,4_Bis(2,4_dinitro phenyl) _3_methyl_ Pyrazole _5_one. The reaction of this compound with various Aldehydes and ketones afforded the bimolecular. The reactions have been monitored by (TLC) and the compounds under study have been identified using the physical constants( melting point and colour) and the available spectrophotometric methods (FTIR, H1-NMR, 13C-NMR) and the results have confirmed the structures of the synthesized compounds.

Part2 : Biological and Enzymic activity The biological and enzymic activity of the synthesized compounds have been evaluated . The evaluation of biological activity was on some types of bacteria which are causing some disease using two methods: 1-The diffusion method 2-The dilution method. The results have been compared with various antibiotics and the activity of the synthesized compound were closely similar to that of these antibiotics. The enzymic activity of some compounds was studied on three types of enzymes which are: 1-Alanine Aminotransferase(ALT). 2-Aspartate Aminotransferase(AST). 3-Alkaline Phosphates(ALK). The results have shown that the compounds containing nitro group activate was activated all these enzymes values in the patients serum, while the compounds without nitro group deactivate the enzymes values of all the studied enzymes .