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Abstract The bioisosteric interrelation between the benzimidazole skeleton and certain structural entities found in many active antimicrobial and antineoplastic agents; such as the pteridine part in folic acid antagonists and the purine moiety in some antimetabolite agents; have initiated the design of novel benzimidazole derivatives as potential chemotherapeutic agents. Some of the suggested compounds (-.) may be correlated to the pteroyl fragment of folic acid. Other newly proposed compounds (-2) have been designed to incorporate the benzimidazole moiety together with certain bioisosteric relatives to natural pyrimidine metabolites. Additionally, some tricyclic benzimidazolo-bridge head nitrogen compounds (ZQ-fl) have been synthesized in trial to investigate their antimicrobial, antiviral and/or antineoplastic activities. The thesis has been divided into the following chapters: Chapter 1: Introduction: This includes a brief survey on some pharmacological aspects of the benzimidazole derivatives such as antihistaminic, anticonvulsant, analgesic, antiinflammatory, anti-ulcer, antisecretory, anthelmintic as well as antimicrobial, antiviral and antineoplastic activities. |