Abstract:
Coumarins are an important class of oxygen heterocycles which have attracted
researchers in recent years because of their diverse pharmacological properties.
Coumarins have important effects in plant biochemistry and physiology, acting as
antioxidants, enzyme inhibitors and precursors of toxic substances. These scaffolds
have long been recognized to possess anti-coagulant, antioxidant, anticancer, antiinflammatory,
lipid lowering, hepatoprotective, antithrombotic, antiviral activities.
Therefore we designed, synthesized and evaluated this class of compounds for various
biological activities.
The thesis entitled “Design and Synthesis of Novel Oxygen Heterocycles as
Versatile Biodynamic Agents” describes our synthetic efforts towards the
development of novel and potential pharmaceutical agents.
The thesis has been organized under five main chapters as summarized below:
The chapter 1 presents available literature comprising important information about
diverse coumarin based scaffolds including drugs, natural products and synthetic
polycycles associated with biological activities has been reviewed.
The chapter 2.1 describes coumarin-dihydropyridine hybrids: Synthesis, in vitro and
in vivo evaluation as anti-osteoporotic agents. Chapter 2.2 describes coumarin-based
fibrates as potential hypolipidemic and anti-adipogenic agents.
The chapter 3.1 describes discovery and synthesis of novel substituted
benzocoumarins as orally active lipid modulating agents. Chapter 3.2 deals with
synthesis and anti-inflammatory activity of novel biscoumarin-chalcone hybrids.
The chapter 4.1 comprises a simple and efficient access to new functionalized 4-
phenacylideneflavenes. The chapter 4.2 describes a novel route to synthesis of
flavones from salicylaldehyde and acetophenone derivatives.
During our course of studies we also observed some miscellaneous results which are
described in chapter 5. The chapter 5.1 describes indole-based fibrates as potential
hypolipidemic and anti-obesity agents. The chapter 5.2 deals with anti-plasmodial
activity of novel keto-enamine chalcone-chloroquine based hybrid pharmacophores
