The rapidly increasing demand of libraries of small molecules for high-throughput screening (HTS) for drug discovery has posed major challenges to the existing synthetic methodologies. In order to produce molecules with high novelty of structures, it is important to identify the main scaffold with drug-like characters and to synthesize a large number of potentially druggable derivatives, based on that scaffold. This book comprises of two parts. Part A describes discovery of new antioxidants of natural and synthetic origin. Screening of several thousand compounds of diverse structures resulted in the identification of several novel compounds with potent antioxidant potential. Part B of this book deals with the development of novel methods to generate the small molecular libraries of sultams (Cyclic sulfonamides). Development of new facile pathways towards skeletally diverse benzofused sultams through Sonogashira–Pauson–Khand and C-arylation pathway towards tricyclic sultams is described. The main focus of this manuscript has been to develop synthetic strategies and to evaluate the antioxidant potential of diverse compounds.