STUDY ON SOME COUMARIN AND THIOCOUMARIN DERIVATIVES

Abstract

It is well known that, coumanns possess numerous biological activities includes antimicrobial, antitumor, anticoagulant, dermal photo­ sensitizing, diuretic, molluscicidal, anthelminitic, respiratory stimulant, vasodilatory and estrogenic activities.

Therefore, our aim of this work is the synthesis of some new derivatives with increasing biological activity than the parent coumarin by introducing some well known biologically active groups. The structure of the new derivatives were confirmed through microanalysis and spectral measurements (JR, 'H NMR and MS spectra). Also, the antiviral, cytotoxic and antimicrobial activities of some new prepared compounds were studied. The thesis is divided into two main parts: the first part includes the synthesis of new coumarin and thiocoumarin derivatives, the second part includes the biological study of some new prepared derivatives.

Part 1: This part includes the synthesis of some new coumarin and thiocoumarin derivatives. 1- Synthesis of some new thiazolidinone and oxadiazoline coumarin derivatives

The parent 4-hydroxycoumarin was allowed to react with ethyl bromoacetate in the presence of anhydrous potassium carbonate to give ethyl(coumarin-4-oxy)acetate (1) which in turn reacted with equimolecular amount of hydrazine hydrate at room temperature afforded coumarin-4- oxyacetic hydrazide (2)