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العنوان
Synthesis and evaluation of biological activity of some new oxazole and thiazole derivatives /
المؤلف
Said, Gehad Ebrahim El-Sayed El-Sayed.
هيئة الاعداد
باحث / جهاد إبراهيم السيد السيد سعيد
مشرف / ايفلين بشري معوض
مشرف / إبراهيم عبدالجليل عبدالسلام
مشرف / أحمد المكباتي محمد
مناقش / محمد م. مشالى
مناقش / هالة م. رفعت
الموضوع
Hippuric acid. Antioxidants.
تاريخ النشر
2018.
عدد الصفحات
196 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
Organic Chemistry
تاريخ الإجازة
01/09/2018
مكان الإجازة
جامعة المنصورة - كلية العلوم - Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 208

Abstract

Part I: Synthesis and biological evaluation of new multifunctional oxazolone derivatives In this study, different series of new compounds containing phenyl benzoate, oxazolone and other various moieties in one structure with expected biological screening were synthesized using 4-formylphenyl benzoate (1) as a starting material in the synthesis of oxazolones according to classical Erlenmeyer method. Then, 4 aminohippuric acid (2b) was utilized in different chemical transforamtions to obtain different heterocyclic compounds containing oxazol-4-one ring 13-19 via the reaction of these products with aldehyde 1 under Erlenmeyer method conditions. In addition, the reactivity of oxazol-4-one derivative 3a towards various types of amines and hydrazines was studied to give oxazolone derivatives 20-24. Biological activity: antioxidant screening of the newly synthesized oxazolone derivatives using [ABTS] method: all the constructed compounds were tested as antioxidant agents. The results indicated that compounds 20, 23 and 24 proved to show good antioxidant screening. Antibacterial activity of the newly synthesized oxazolone derivatives: The results showed that, compounds 19, 20, 22d and 23 exhibited good activities against Escherichia coli and compounds 19, 20, 22a, 22c, 22d, 23 and 24 showed good activities against Staphylococcus aureus. Part II: Synthesis and antibacterial activity of some new thiazole and thiazolidinone derivatives Cyanoacetyl hydrazone 25 and thiosemicarbazone 29 were utilized in the synthesis of thiazole derivatives 27, 28 and 30-33. Furthermore, three arylidine thiazolidin-5-one derivatives 35 (a-c) were synthesized via the reaction of aldehyde 1 with compounds 34 (a-c). Moreover, pyridinone derivatives 39 (a-d) and 41 (a-c) were obtained through the Michael addition of arylidine cyanoacetamide derivatives 37 (a-d) with malononitrile and ethyl acetoacetate, respectively.Biological activity: all new thiazole derivatives were subjected to antibacterial screening. The results showed that, compounds 27, 29, 30 and 32a showed potent activity against S. aureus bacteria and compounds 30 and 32a showed excellent activity against E. coli bacteria.