Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 3, Pages 1241-1244Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.136
Keywords
AT(1) receptor antagonist sartan
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A series of selenophene analogues of the thiophene-containing anti hypertensives milfasartan and eprosartan were prepared and tested for AT(1) receptor antagonist properties. All four selenophene compounds proved to be potent AT(1) receptor antagonists, with pK(B) estimates indicating that these selenides are at least as effective as the thiophene parent compounds at blocking AT(1) receptor mediated responses. These results reveal that replacement of sulfur with selenium in thiophene-containing sartans does not interfere with sartan activity. (C) 2007 Elsevier Ltd. All rights reserved.
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