Synthesis and pharmacological characterization of novel N & O containing heterocyclic compounds as potential therapeutic agents

The majority of pharmaceuticals and biologically active agrochemicals are heterocyclic compounds; it represents their immense importance in serving mankind. The purpose of this thesis was to investigate feasibility of making potential biological active noval heterocyclic compounds designed based on lead molecules. The work accomplished in this thesis includes five different chapters to explain importance, achieve simple and fused-ring heteropolicyclic systems having potential pharmacological properties. The first chapter briefly explains importance of heterocyclic compounds and research objective. The second chapter of thesis concerns with target-oriented synthesis to access complex dehydro shikimate analogues containing a pyridine/isoquinoline unit with antitubercular activities with MIC: 4-10μM. Third chapter deals with study of novel synthetic approach to the one pot synthesis of 2H-benzo[b] [1,4]oxazines with anti inflammatory activites. In the fourth chapter is presented as a series of functionalized phenyl oxazole derivatives were designed, synthesized and screened in vitro for their activities against LSD1 and for effects on viability of cervical and breast cancer cells (IC50: 1-10 nM), and in vivo for effects using zebrafish embryos. Indeed it also explains the designing and cost effective route to synthesis of LSD1 inhibitors. Finally, fifth one is related to the intramolecular 1,3-dipolar cycloaddition of isovanillin derived N-aryl hydroxylamines possessing ortho-allylic dipolarophiles affords novel benzo analogues of tricyclic isoxazolidines that can be readily transformed into functionalized lactams, γ-aminoalcohols and oxazepines. The corresponding N-unsubstituted hydroxylamines give rise to tetrahydroisoquinolines. Anxiogenic properties of these compounds were tested in zebrafish. Moreover, in all chapters in silico docking studies were performed to predict binding interactions of the most potent scaffolds synthesized and reported inhibitors with the selected targets. At the end of each chapter are drawn a series of conclusions, concerning the investigations performed and the results obtained