الفهرس 
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Abstract
SUMMARY
”Use of carbazone derivatives in the synthesis of nitrogen heterocycles and their biological activity”
This thesis focused on the use of carbazone derivatives in the preparation of Nitrogen heterocycles such as 2-thiohydantion and 1,3-thiazole derivatives and study the chemical reactions of some prepared nitrogen heterocycles and their biological evaluation against anticancer activity.
The thesis includes four main chapters as follow:-
Chapter one: “Literature Survey”
This chapter containing the literature survey on the synthesis and chemical reaction of nitrogen heterocycles (such as 2-thiohydantion and thiazole derivatives) from the last year.
Chapter two “Results and Discussion”:
The search work in this chapter focused on use of 2,3-dihydroxybenzaldehyde thiosemicarbazone (2) in the preparation of 2-thiohydantion and 1,3-thiazole derivatives as a key starting material. All of the synthesized nitrogen heterocycles have been characterized by IR, 1H-NMR, 13C-NMR, mass spectrometry and elemental analyses.
This chapter divided into two parts as the following:-
Part one: synthesis of Novel 2-thiohydantion derivatives.
3-[(2,3-dihydroxybenzylidene)amino]-2-thiohydantion (3) was prepared via the cyclization of thiosemicarbazone derivatives (2) with ethyl chloroacetate in presence of fused sodium acetate.
Acetylation, addition and condensation reactions of the 2-thiohydantion (3) with acetic anhydride, methyl acrylate in dimethyl formamide and benzaldehyde in the presence of base yielded the corresponding triacetoxy derivatives (4), methyl 3-substituted-2-thiohydantion-1-yl-propionate (5) and benzylidene derivative (7). Condensation of compound (5) with benzaldehyde yielded the benzylidene derivative (6). Acetylation of benzylidene derivatives gave diacetoxy derivative (8, Scheme 1).
Part two: synthesis of substituted 1,3-thiazole derivatives.
Substituted-1,3-thiazole derivatives (9 and 10) were prepared via the cyclocondensation of thiosemicarbazone (2) with aryl bromomethyl ketones under different condition reaction.
Acetylation, alkylation, condensation and halogenation reactions of substituted-1,3-thiazole derivatives (9 and 10) with acetic anhydride, methyl iodide, aromatic aldehydes and bromine in acetic acid led to the formation of diacetoxy derivatives (11 and 12), N-alkyl derivatives (13 and 14), vinyl azo compounds (22). Acetylation of N-alkyl derivatives (13 and 14) and 2-(substituted) azo-1,3-thiazole (22) with acetic anhydride gave diacetoxy of N-alkyl derivatives (16 and 17) and diacetoxy derivatives of 2-azo-1,3-thiazole (23, Scheme 2).
Also, in the chapter two containing the investigation of mass spectrometry for the synthesized Nitrogen heterocycles such as 2-thiohydantion and 1,3-thiazole derivatives, since this can be used to confirm or to obtain the relative molecular mass. The molecular ion of some synthesized Nitrogen heterocycles are dissociated to smaller fragments. By examining the fragments and by knowing the classes of molecules dissociate on electron impact, one can deduce the structure of the prepared compounds.
Chapter three: “Biological Evaluation”
2-thiohydantion and 1,3-thiazole derivatives were screened for antitumor activity. Some of the prepared Nitrogen heterocycles showed significant antitumor activity. Also, some compounds showed high antitumor activity compared to other compounds.
The evaluation results of some Nitrogen heterocycles against antitumor activity are summarized in Table 3, 6, 9 and 12.
Chapter Four: “Experimental Part”
In this chapter four containing the procedures of the practical experimental with deals for the syntheses of 3-substituted-2-thiohydantion derivatives and substituted-1,3-thiazole derivatives. Also, this chapter contain the instrument which used in the analysis of some prepared Nitrogen heterocycles (such as Infrared, Nuclear Magnetic Resonance and Mass Spectrum) and Elemental Analyzer.