URACIL-BASED ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
DORSCH D MEDERSKI WWKR OSSWALD M BEIER N SCHELLING P
Citation
D. Dorsch et al., URACIL-BASED ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(18), 1995, pp. 2071-2076
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
18
Year of publication
1995
Pages
2071 - 2076
Database
ISI
SICI code
0960-894X(1995)5:18<2071:UARA>2.0.ZU;2-E
Abstract
1,2,3,4-Tetrahydro-2,4-pyrimidinedione (uracil) is a valuable nucleus for the construction of potent antagonists of the AT(1) angiotensin II receptor. Various synthetic routes were applied in order to introduce a wide range of different groups at the N-3-nitrogen and to obtain co ndensed uracil derivatives as well. 121 with a N,N-dimethylacetamide r esidue at N-3 was the most potent compound with an IC50 of 0.65 nM.