Fluorescent Angiotensin AT1 Receptor Antagonists

Fluorescent selective angiotensin AT(1) receptor antagonists (sartans) that contain naphthalene (6, 7, 10, and 11), anthracene (12 and 14), acenaphthene (13 and 15), and coumarin (8 and 9) substituents have been prepared and their preliminary pharmacology evaluated in Chinese hamster ovary (CHO) cell based assays. Compounds 6-15 proved to be effective sartans with pK(B) estimates in the range of 6.7-10.5; their potential as cellular imaging agents is also discussed.