الفهرس 
INTRODUCTIONOnly 14 pages are availabe for public view
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Abstract
Azole derivatives contribute for a wide range of biological activities especially as antimicrobial, anticancer and anti-inflammatory.
This fact motivated us to design and synthesize some novel azole ring system (pyrazole, oxadiazole, thiadiazole and triazole) linked to thienopyrimidine scaffold carried at position 2 or 3. Some selected candidates of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tumor cell lines. In addition, all the newly synthesized compounds were investigated for their antimicrobial activities. The present thesis comprises the following chapters:
Chapter I: Introduction:
It includes a brief survey of the literature concerning biologically active azole derivatives with antimicrobial, anticancer and anti-inflammatory activities and presents the aim of the work and the basis on which the newly suggested compounds have been synthesized.
Chapter II: Discussion:
Discusses the adopted synthetic routes used to achieve the target compounds. The thesis comprises four synthetic schemes illustrating the different reaction pathways followed in the synthesis of the target compounds
Scheme 1:
Describes the synthesis of ethyl 2-amino-5-carbamoyl-4-methylthiophene-3-carboxylate 1 and its cyclization to the corresponding thienopyrimidine derivatives 2 or 5 either through reaction with benzylisothiocyanate or formamide, respectively. Alkylation of 2 and 5 with ethyl bromoacetate followed by reacting the obtained esters 3 and 6 with hydrazine hydrate gave the two key intermediate acid hydrazide derivatives 4 and 7, respectively.
Scheme 2:
Involves the condensation of the acid hydrazide 4 with the appropriate aromatic aldehyde, 3-Aryl-1-phenyl-1H-pyrazole-4-carbaldehydes or isatin to afford the corresponding hydrazones 9a-c, 10a-d and 11, respectively. In addition, we attempted to prepare the pyrazolidine-3,5-dione and pyrazol-5(4H)-one derivatives by condensation of the acid hydrazide 4 with diethyl malonate and benzoyl chloride, followed by treatment of the obtained intermediates 12 and 14 with sodium ethoxide and sodium hydroxide, respectively, but instead the S-alkyl side chain was replaced by 2-ethoxy 13 and 2-hydroxy 15 groups.