The greatest challenge facing our global future today is ‘Health’. To have a better living standard, a growing world population will need easily available and cheaper medicament, especially in metabolic disorder diseases (Cancer, Type-2 diabetes & etc.) and infectious diseases. To combat this impending situation, discovering of novel molecules with unmet physiochemical properties are needed especially in the area of endemic metabolic disorder and infectious diseases. Novel bioactive molecules can be developed by combining basic research with applied science keeping in mind that chemistry is central to everything. This talk will place the scale of the global medical issue in perspective and then discuss some of the issues related to basic science that is needed to emulate drug discovery. With this basic science in place, the design and synthesis of desired compounds and their application to cure diseases through controlling the cell fate in vitro and in vivo will be presented.