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العنوان
Synthesis of some new Heterocycle-Amino Acid Conjugates of Pharmaceutical Interest /
المؤلف
Agha, Khalid Abd-Elhay Mahmoud Badr.
هيئة الاعداد
باحث / خالد عبدالحى محمود بدر أغا
مشرف / إعتدال حسن عبدالعال
مشرف / نادر المغاورى مصطفى
مشرف / طارق محمد صلاح
الموضوع
Amino Acids- Synthesis- Congresses.
تاريخ النشر
2016 .
عدد الصفحات
156 P. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
العلوم الصيدلية
الناشر
تاريخ الإجازة
1/1/2016
مكان الإجازة
جامعة الزقازيق - كــليـــة الصيدلــــة - Organic Chemistry
الفهرس
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Abstract

The synthesis of N-acylbenzotriazoles and their potential in a number of organic transformations are reviewed.
A novel and efficient synthesis of N-acylbenzotriazoles (Ia-m, IIa, Va, VIa, VIIa, VIIIc and Xa) from the corresponding carboxylic acids and tosyl chloride is discussed. This methodology is used for the synthesis of Vorinostate (SAHA) III, new N-acyl derivatives of Cephalexin (IXa-k’) and N-(3-nicotinamidobenzoyl) aminoacids (XIa-m).
The antibacterial activities of N-acylcephalexins were evaluated against Staphylococcus aureus (ATCC 6538), Paenibacillus polymyxa (ATCC, 842), Escherichia coli (ATCC 10536) and Pseudomonas aeruginosa (ATCC 27853).
N-(3,4,5-Trimethoxybenzoyl)cephalexin (IXb) and N-Cbz-Trp-cephalexin (IXg) exhibited a broader spectrum antibacterial activity.
Cytotoxicity of N-(3-nicotinamidobenzoyl)amino acids (XIa-m) was tested against breast (MCF-7), colon (HCT-116) and prostate carcinoma (DU145 and PC3) cell lines. Compounds XIh, XIj, and XIk showed cytotoxic activities higher than 5-Fluorouracil (5-FU) against breast carcinoma cell line (MCF-7) and higher than 5-FU and Imatinib incase of colon carcinoma cell line. Most of the synthesized compounds XIa-m exhibited good cytotoxic activity against prostate carcinoma cell lines DU-145 and PC3.