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تحضير وتشخيص ودراسة الفعالية البايوكيميائية لبعض مشتقات ? لاكتام
Author name:
عذراء محمد علي
Supervisor name:
علي هاشم عيسى | سميرة احمد زيارة
General topic:
Chemistry
Specific topic:
Chemistry
Degree:
Master
University:
University Of Basrah - College Of Science - Chemistry Department
Language:
Arabic
University location:
Basrah
First pages:
25T1593 - p.pdf
Abstract:
The Staudinger reaction of imines to β - lactams was successfully achieved using chloroacetyl chloride and tertiary amines in dry toluene under mild conditions. Two new types of β - lactams have been synthesized by this versatile and efficient method in good to excellent yields.R2 R1 الرمز Br NO2 A CN NO2 M OCH3 OCH3 F Br OCH3 B The imines were synthesized according to the literature procedure by reaction of substituted aldehydes and substituted anilines.The chloroacetyl chloride has been synthesized by the reaction of chloroacetic acid with phosphorus pentachloride (PCl5) and used directly with out any purifications.All products were characterized using IR, H and C NMR. This method is simple, clean, and the by - products were removed by simple aqueous work - up. The effects of solvents, molar ratio of reagent, and the temperature were considered.The antibacterial acttivity of the compounds A, M and F has been studied on gram positive isolates (Staphylococcus aureus and Bacillus) and gram Negative isolates (E. coli and Psedomonas), in comparison with standard antibiotics which are : Ampicillin, Amoxicillin and Cephalexin.The results showed the influence of the effectiveness of inhibitory compounds on all bacterial isolates at concentration (250 mg / ml). The study also included the estimation of minimum inhibition concentration of these compounds at all examined bacterial isolates. The results showed the contentiously effectiveness of the compounds (A, M) in the inhibition of the gram positive Staphylococcus aureus spp. up to focus (25 μg / ml). In addition, our study includes determination of the effect of compounds A, M and F on human fresh red blood cells as cytotoxicity in concentrations (1,5,25,50,250 mg / ml). The results were revealed that there was non - hemolysis of red blood cells, so it can be considered these compounds are non - toxic on the human red blood cells.The effect of studied compounds (A, M, F) at concentrations (50, 125, 250 mg / ml) dissolved in DMSO solution, were determined to detect the symptoms of hypersensitivity test using the domestic rabbits, no appearance of any symptoms were observed for hypersensitivity Lalani swelling and redness, or itching after injection of these compounds for the first time, as well as after the exposure to these compounds after Done week measure, the level of antibodies type lgE and white blood cells type acidic Eosinophil, were measured after injection of these compounds which not get any significan
