Synthesis and Biologieal Investigation of Some Phthalazine Derivatives

Abstract

It is well-documented that phthalazines and more precisely triazolophthalazines possess broad spectrum of biological interest especially antihypertensive, anticancer, antimicrobial and anti• inflammatory activities. Based on the • above-mentioned information, different senes of compounds were synthesized in this thesis containing various heterocyclic moieties joined or fused to phthalazine or triazolophthalazine ring systems to be screened for their antihypertensive, anticancer, anti-inflammatory and /or antimicrobial activities, The present thesis comprises the following chapters. Introduction:

It constitutes a concised survey on the recent researches on biologically active phthalazines as antihypertensive, anticancer, antimicrobial, antiviral, anti-inflammatory, analgesic, antidiabetic, antihistaminic, anticonvulsant agents and many others. Research objectives:

It deals with the rationale upon which the synthesized compounds have been designed. Results and Discussion:

This chapter includes a discussion of the theoretical basic concepts for the • already reported acceptable methods for the synthesis of the designed compounds, referring to the available knowledge in the literature. This necessitated a survey of the reported methods utilized for the preparation of compounds of comparable structures .. This chapter is subdivided into five parts: Part I: It describes preparation of the key intermediate 3-methyl-

1,2,4-triazolo[3,4-a]phthalazin-6(5H)-one and its reaction with 1,3-diaryl•

pyrazole-4-carbaldehydes, 4-substituted benzaldehydes and arylglyoxal