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Bromobenzofurans : a new class of potent, non-peptide antagonists of angiotensin II |
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| Authors: | D Middlemiss G M Drew B C Ross M J Robertson D I C Scopes M D Dowle J Akers K Cardwell K L Clark S Coote C D Eldred J Hamblett A Hilditch G C Hirst T Jack J Montana T A Panchal J M S Paton P Shah G Stuart A Travers |
| Institution: | Glaxo Group Research, Ware, Herts, SG12 0DJ, UK |
| Abstract: | This paper describes the synthesis and pharmacology of a novel series of benzofurans which are antagonists of angiotensin II. One of these, the bromobenzofuran 11b, is a potent (apparent pKB=9.8) and specific antagonist of angiotensin II which, after oral administration (10mg/Kg), causes marked and long-lasting ( > 24h) falls in blood pressure in renal hypertensive rats. |
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