Uracil-based angiotensin II receptor antagonists

1,2,3,4-Tetrahydro-2,4-pyrimidinedione (uracil) is a valuable nucleus for the construction of potent antagonists of the AT1 angiotensin II receptor. Various synthetic routes were applied in order to introduce a wide range of different groups at the N3-nitrogen and to obtain condensed uracil derivatives as well. 121 with a N,N-dimethylacetamide residue at N3 was the most potent compound with an IC50 of 0.65 nM.