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العنوان
Access to Convenient Synthesis and Biological Screening of Some Nitrogen Heterocycles \
المؤلف
Khalifa, Aya Mahmoud Abd-elrahman.
هيئة الاعداد
باحث / آية محمود عبد الرحمن خليفة
مشرف / سامح أحمد محمد أحمد رزق
مشرف / عبدالجواد علي فهمي
مشرف / إيمان عبدالرحمن السيد حسن الحلو
تاريخ النشر
2023.
عدد الصفحات
280 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
Chemistry (miscellaneous)
تاريخ الإجازة
1/1/2023
مكان الإجازة
جامعة عين شمس - كلية العلوم - الكيمياء
الفهرس
Only 14 pages are availabe for public view

from 280

from 280

Abstract

Part I:
The broad spectrum of biological activity of pyrazole derivatives coupled with our interest in the chemistry of nitrogen heterocycles, led us to synthesize a bis-benzoxazinone derivative bearing a pyrazole scaffold and utilize it as a key material for the construction of some bisimidazole, bistriazole and bisbenzimidazole derivatives obtained by reactions with some mono- and bidentate nitrogen nucleophiles. The density functional theory studies of the synthesized compounds were calculated. The synthesized compounds were screened for their in vitro antiproliferative activity against two human tumors; HePG2 and MCF-7. Some compounds displayed satisfactory activities.
Part II:
The highly functionalized, pyrazolylmalonyl diisothiocyanate derivative was synthesized and treated with some nitrogen nucleophies like 4-acetylaniline, 2-aminobenzoic acid, 6-aminothiouracil, 2-aminothiadiazole derivative, hydrazine, phenylhydrazine, thiophene-2-carbohydrazide, 2-hydroxybenzohydrazide, 2-cyanoacetohydrazide, thiourea, thiosemicarbazide, 2-aminoaniline, and thiocarbohydrazide. The synthesized compounds were screened for their insecticidal activity against healthy late third instar larvae P. interpunctella and Nilaparvata lugens and the results showed that some of them were of promising potency that are supported by DFT stimulation and their molecular docking.
Part III:
A new series of various N-(1-(2-chlorobenzo[h]quinolin-3-yl)-1-substituted-vin-2-yl)benzamide derivatives was designed and synthesized based on the 2-chlorobenzo[h]quinoline core as potential antioxidant and insecticidal agents. In vitro antioxidant activities of these compounds were evaluated and compared with commercial antioxidant (ascorbic acid). The results showed good antioxidant activities of these compounds. In addition, in vitro insecticidal activities revealed that most of these compounds exhibited high insecticidal activity against cotton leafworm compared with chlorpyrifos. Some compounds in these series were better than the commercial insecticidal, chlorpyrifos.