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العنوان
Synthesis and characterization of Novel Heterocyclic
Compounds with their Anticipated Biological Activity /
المؤلف
Mohamed, Asmaa Semida Taha.
هيئة الاعداد
باحث / أسماء صميدة طه محمد
مشرف / إبراھيم السيد محى الدين
مشرف / رضا نصر متولي
مشرف / رضا فتحى الشعراوي
مناقش / سمية متولي الدسوقي
مشرف / جيهان عبدالرازق حسنين
الموضوع
Novel Heterocyclic. Anticipated Biological.
تاريخ النشر
2014.
عدد الصفحات
136 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الكيمياء
الناشر
تاريخ الإجازة
1/3/2014
مكان الإجازة
جامعة السويس - المكتبة المركزية - الكيمياء
الفهرس
Only 14 pages are availabe for public view

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Abstract

This thesis is divided into three chapters, introduction, synthesis of some
heterocyclic imidazolidine compounds and biological activity of some nitrogen
heterocyclic compounds.
Chapter I: Introduction
This chapter contains literatures review of imidazolidinone derivatives for the
last years.
Chapter II: Synthesis of some nitrogen heterocyclic compounds
This chapter deals with the synthesis of thiohydantoin derivatives.
The author tend to synthesis of thiohydantoins starting from 1-acetylferrocene
(1) that was converted into the corresponding 1-[(ferrocene-1-
ylethylidene)amino]-thiourea (2) using thiosemicarbazide. Treatment of the
thiourea derivative (2) with ethyl chloroacetate yield the corresponding 3-
[(ferrocene-1-ylethylidene)amin o]-2-thioxo-imidazolidine-4-one (3).
Furthermore, compound (2) undergoes coupling reaction with phenacyl bromide
in the presence of fused sodium acetate in acetic acid to give the corresponding
4-phenyl-3-[(ferrocene-1-ylethylidene)amino]-imidazolidine-2-thione (4) which
was converted to 1-acetyl-3-[(ferrocene-1-ylethlidene)amino]-4-phenylimidazolidine-2-thione (8) via the actylation with acetic anhydride (Scheme 1).
Ferrocenyl-thiohyantoin (3) was either converted into the 1-acetyl-3-
[(ferrocene-1-ylethylidene) amino]-4-hydroxy-imidazolidine-2-thione (5)
through boiling in acetic anhydride or reacted with two different aromatic
aldehydes (a, b) in piperidine to yield the corresponding ferrocenyl-thiohyantoin arylidenes, 3-[(ferrocene-1-ylethylidene) amino]-2-thioxo-5-
arylidene-imidazolidine-4-ones (6a, b). The ferrocenyl-thiohyantoin arylidenes
(6a, b) were further acetylated with acetic anhydride to afford the corresponding
1-acetyl-2-thioxo-3-[(ferrocene-1-ylethylidene)amino]-5-arylideneimidazolidine-4-ones (7a, b) (Scheme 2).
Chapter III: Biological activity of some nitrogen heterocyclic compounds
Antimicrobial activities of the prepared compounds (2-8) were investigated
using agar well diffusion method. Antibacterial activity was studied against the
bacillus subtilis and staphylococcus aureus as gram positive bacteria, while
Escherichia coli and pseudomonas aeruginosa as gram negative bacteria.The
zone of inhibition was measured compared with standard drug (ciprofloxacin).
The inhibition zone was measured compared with fluconazole as standard drug,
and using DMSO as a blank as antifungal activity. The cytotoxic activities of
prepared compounds were tested against HepG-2 cell line according to method
of Masmann and Vijayen et al.
Compounds 2 and 4 showed antitumor activity than the standard antitumor drug
against HepG-2 cell line.