Synthesis of Pharmacologically Active Kinase Inhibitors
Megjelenés dátuma: 2021-05-17
Kulcsszó: organic chemistry
medicinal chemistry
heart failure
kinase inhibitor
structure-activity relationship
thieno[2,3-c]pyridine scaffold
functionalization
szakdolgozat
medicinal chemistry
heart failure
kinase inhibitor
structure-activity relationship
thieno[2,3-c]pyridine scaffold
functionalization
szakdolgozat
Absztrakt:
A series of GRK2 kinase inhibitors were designed based on hits after the high throughput screening. The aim was to optimise a kinase inhibitor in order to treat heart failure. Thieno[2,3-c]pyridine derivatives were synthesized and tested on pharmaceutical assays. Both activity and lipophilic ligand efficiency was improved. Further functionalization of thieno[2,3-c]pyridine scaffold was carried out.