Synthesis and pharmacological evaluation of benzimidazole derivatives of isoxazoline-5-one pyrazoline-5-one and pyrazolidine-3, 5-dione compounds

Abstract

The thesis entitled Synthesis and Pharmacological Evaluation of Benzimidazole Derivatives of Isoxazoline-5-One, Pyrazoline-5-One and Pyrazolidine-3,5-Dione compounds is divided in to four Chapters. Chapter 1 contains an over view of the heterocyclic compounds such as benzimidazoles, newlineisoxazolines, pyrazolinones and pyrazolidine-3,5-diones. Chapter 2 describes about synthesis of new benzimidazole derivatives containing isoxazoline-5-one, pyrazolin-5-one and pyrazolidine-3,5-dione. Chapter 3 dealing on docking studies of the newly designed compound for screening their antibacterial, antifungal and anti-inflammatory activities with the help of docking software such as HEX, and Autodock. Chapter 4 describes studies on the biological activity such as antibacterial, antifungal, anti-inflammatory along with ulcerognic activity and invitro anti-oxidant activities of new compounds reported in this thesis. Chapter 1: Introduction This chapter mainly attempted to bring out some of the highlights of heterocyclic compounds particularly importance of benzimidazole, isoxazole, pyrazolines and pyrazolidine-3,5-dione, from literature. This chapter reviews the medicinal importance of these nuclei. The present work explains synthesis and chemistry of benzimidazole, pyrazoline and pyrazolone, isoxazole derivatives, and their biological importance such as antimicrobial, antifungal, antiviral, anti-diabetic, anti-cancer, anti-ulcer and antiinflammatory properties. An attempt has been made to bring out the medicinal importance these heterocyclic compounds. newlineChapter 2: This chapter deals with the synthesis of new benzimidazole derivatives containing isoxazoline-5-one, pyrazoline-5-one, N-phenyl pyrazoline- 5-one and pyrazolidine-3, 5-dione. In scheme-1, 2-substituted benzimidaozles 2 (a-e) are prepared and coupled with 4-amino benzoyl chloride (1) in the presence of potassium carbonate and then converted in to its diazonium salts and coupled with ethyl acetoacetate and diethyl malanoate.