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 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.
Grange
Rebecca L
RL
School of Chemistry, The University of Melbourne, Vic. 3010, Australia.
Ziogas
James
J
North
Andrea J
AJ
Angus
James A
JA
Schiesser
Carl H
CH
D000179:Acrylates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047228:Angiotensin II Type 1 Receptor Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D005260:Female; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D016566:Organoselenium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D010053:Ovary / Q000166:cytology; D044140:Receptor, Angiotensin, Type 1 / Q000378:metabolism*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry / Q000493:pharmacokinetics; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
D000179:Acrylates; D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D007093:Imidazoles; D016566:Organoselenium Compounds; D044140:Receptor, Angiotensin, Type 1; D013876:Thiophenes; C068373:eprosartan; D013455:Sulfur; C527223:milfasartan