Selenosartans: Novel selenophene analogues of milfasartan and eprosartan

A series of selenophene analogues of the thiophene-containing antihypertensives milfasartan and eprosartan were prepared and tested for AT1 receptor antagonist properties. All four selenophene compounds proved to be potent AT1 receptor antagonists, with pKB estimates indicating that these selenides are at least as effective as the thiophene parent compounds at blocking AT1 receptor mediated responses. These results reveal that replacement of sulfur with selenium in thiophene-containing sartans does not interfere with sartan activity.

The synthesis and preliminary evaluation of selenophene-containing sartans (e.g. 4; pKB = 8.3) is reported.Figure optionsDownload as PowerPoint slide