The dissertation thesis comprises a chapter describing medicinal chemistry case study and another chapter focused on the development of synthetic methodologies for medicinal chemistry. The medicinal chemistry case study is directed to the development of non-steroidal anti-inflammatory drugs with a new mechanism of action. The pharmacological target in the study is microsomal prostaglandin synthase 1 (mPGES-1). Computer modelling along with traditional structure-activity relationship (SAR) studies has been used in the design of the enzyme inhibitor. Development of a pharmacophore model facilitated the development of inhibitors and the work has resulted in several lead structures for further in vivo studies. The intellectual contribution in the development of mPGES-1 inhibitors is summarized in 4 international patent applications. The synthetic methodology part of the dissertation thesis is directed toward the development of new organic synthesis methods for the late–stage functionalization of a lead structure in drug discovery. The thesis summary provides a general overview of the complete work.