2. Academic Validation
  3. Selenosartans: novel selenophene analogues of milfasartan and eprosartan

Selenosartans: novel selenophene analogues of milfasartan and eprosartan

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):1241-4. doi: 10.1016/j.bmcl.2007.11.136.
Rebecca L Grange 1,  James Ziogas,  Andrea J North,  James A Angus,  Carl H Schiesser
Affiliations

Affiliation

  • 1 School of Chemistry, The University of Melbourne, Vic. 3010, Australia.
PMID: 18191398 DOI: 10.1016/j.bmcl.2007.11.136
Abstract

A series of selenophene analogues of the thiophene-containing antihypertensives 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.

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