Systemic and Gastrointestinal Tract Directed Protease Activated Receptor-2 Modulators

Protease activated receptor 2 (PAR2) is a distinctive member of a rare family of G-protein-coupled receptors. PAR2 plays a vital role in multiple different types of diseases, including fibrosis, cancer, and other immune and inflammatory diseases. Thus, it acts as an important prospective drug target. Most of the PAR2 antagonists reported to date lack potency, selectivity, or other drug-like properties. Hence, there is a need for potent, orally bioavailable, receptor and pathway-selective analogues to treat PAR2-mediated diseases. This thesis describes the development of in vivo tool compounds with excellent drug-like properties.