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Abstract
It is well-documented that pyrimidines as well as triazolopyrimidines occupy a wide space of biologically active compounds especially in the field of anticancer and antimicrobial activities. This fact innovated the design and synthesis of ninty novel pyrimidine derivatives bearing various substituents or heterocyclic moieties joined or fused to the pyrimidine ring system. Some selected members of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tumor cell lines as well as their antimicrobial activities.
The present thesis comprises the following chapters:
Chapter I: Introduction
It includes a brief survey of the most recent publications on biologically active pyrimidines possessing anticancer, antiviral, antimalarial, antimicrobial, anti-inflammatory as well as other activities.
Chapter II: Research objectives
It deals with the aim of the present work and the rationale upon which the newly suggested compounds have been designed.
Chapter III: Discussion
This chapter includes, the theoretical concepts of the methods adopted for the synthesis of the designed compounds with reference to the knowledge available in literature. Some chemical reaction mechanisms have been proposed to account for some of the given products. The following schemes give illustrative information:
Scheme 1:
It describes the different procedures adopted for the preparation of the synthones; 6-substituted-4-oxo-2-thioxo-1,2,3,4-tetrahyDROPyrimidine-5-carbonitriles 1a-c and their different 2-thioethers 2a-c, 3a,b and 7a,b derivatives. It deals also with the conversion of 2a into the corresponding cyclic phosphochloridate derivative 4.
Furthermore, substitutedamino derivatives 6a-i were obtained by allowing the synthones 1a-c to react with phosphorous oxychloride to yield the chloro compounds 5a-c which were further reacted with the proper secondary amine.
Scheme 2:
It comprises treating the synthones 1a-c with p-substituted chloroacetanilides 8a,b to furnish the corresponding thioacetamido derivatives 9a-d. Furthermore, our synthones 1a-c were converted to the corresponding substituted amino derivatives 11a-f via the corresponding thiomethyl intermediates 10a-c. The latter were employed for the preparation of hydrazine derivatives 12a-c which, in their turn, were converted to pyranopyrazoles 13a,b and triazolopyrimidine derivative 14 by treating separately with diethyl malonate and ethyl cyanoacetate respectively. The open chain counter-part of 14, namely; ethyl 3-substituted iminopropanoate derivative 15 was also obtained.