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Abstract
The present investigation deals with the semi-synthesis of certain 1,3,4- trisubstituted pyrazole derivatives derived from the natural furochromone khellin, to be screened for their in vivo anti-inflammatory activity and ulcerogenic liability hoping to obtain anti-inflammatory agents with high potency and lower side effects. Furthermore, PGE₂ and TNFÜ immunoassay were carried out to determine the percentage inhibition of these factors by the most active tested compounds. Docking study was conducted for the tested compounds on the active site of COX-2 enzyme to study the binding mode in the active site of the enzyme.The thesis consists of the following parts: 1.Introduction: In this section, literature review about the various biological and pharmacological activities especially the anti-inflammatory activity of pyrazole, pyrazoline, benzofuran and chalcone derivatives was presented. Also, different reported methods for the preparation of both pyrazole and pyrazoline nuclei were described