The objective of drug discovery phase is to synthesize lead compounds, new analogs with improved potency, reduced off target activities, and physiochemical/metabolic properties suggestive of reasonable in vivo pharmacokinetics. This optimization is accomplished through empirical modification of the hit structure and/or by employing structure-based design if structural information about the target is available. The goal of present work is to design drug with minimum side effect and maximum potency. 2D QSAR is planned using Multiple Linear Regression Analysis, for achieving the goal, which can help in recognizing the important descriptor that can help in increasing the potency of anticancer drugs.

In current drug discovery and development field bioanalytical techniques plays an important role in quantitative determination in plasma. Various pharmacokinetics, toxicokinetics, bioequivalence and exposure-response (pharmacokinetics/ pharmacodynamics) are biomedical drug development pursuits that cannot be accomplished without an accurate means of quantifying the moieties that scientists seek to characterize. Many chromatographic techniques immensely used for this. Hence this book comprehensively gives an overview on various important aspects and challenges in bioanalytical techniques. Beside this it also enlighten bioanalytical method validation which gives regulatory requirement for any process.

The resistance of malaria parasites to widely used drugs prompted an upsurge in the development of new drugs with novel mechanism of action, and re- evaluation of the existing drugs to overcome the resistance problem. A number of new potential target pathways have already been identified and efforts to develop lead compounds for these putative targets hopefully will allow treatment of malaria infections in a uniform sustained way. Considerable research efforts were directed in the areas of chloroquine drug resistance reversal agents. Careful development of some bisquinolines, which are free of toxic side effect, 4-anilinoquinolines and modified chloroquine analogs may be helpful to obtain drug candidates that inhibit the growth of chloroquine sensitive and resistant parasites. In the past several years, new structural classes of antimalarial agents, target based antimalarial agents, iron chelators have made some interesting and promising lead molecules available for further optimization to provide compounds for clinical development.

Pulsatile Drug Delivery Systems are gaining a lot of interest as these systems deliver the drug at specific time as per the pathophysiological need of the disease, thus providing spatial and temporal delivery and increasing patient compliance. Diseases wherein such delivery systems are promising include asthma, peptic ulcer, cardiovascular diseases, arthritis, attention deficit syndrome in children, and hypercholesterolemia. This book will cover various approaches that have been developed to control drug delivery profile with different polymeric systems like time controlling, internal stimuli induced (temperature induced and chemical stimuli-induced), external induced (magnetic fields, ultrasound, electric fields and light stimulation) and Multiparticulate system. Special attention have been made towards recent advances, patents, future opportunity and major challenges regarding formulation of pulsatile drug delivery of oral dosage forms and are summarized and discussed.