Abstract
The angiotensin-converting enzyme 2 (ACE2) is pivotal as the cellular receptor for SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2), the virus responsible for COVID-19. This study presents a novel synthetic route for four analogues of MLN-4760, a known inhibitor of ACE2, guided by in silico docking predictions. These synthetic advances enabled in vitro pIC(50) assays confirming the inhibitory potency of the synthesized analogues. Lastly, this route was applied to the synthesis of novel (18)F-labeled ACE2 inhibitors for PET imaging applications.