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[Angiotensin II receptor antagonists: candesartan cilexetil].

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan (2001-02-24)
T Naka, K Kubo, K Nishikawa, Y Inada, Y Furukawa
ABSTRACT

Blockade of the action of angiotensin II (AII) has long been a target for the development of novel antihypertensive agents. We recently discovered a novel class of potent nonpeptide AII receptor antagonists, benzimidazole-7-carboxylic acids including candesartan. Candesartan is a highly potent and insurmountable AII type-1 receptor (AT1)-selective antagonist. Structure-activity relationship (SAR) studies revealed that the adjacent arrangement of a lipophilic substituent, a tetrazolylbiphenylmethyl moiety and a carboxyl group was the important structural requirement for potent AII antagonistic activity. Especially, the presence of a carboxyl group at the 7-position was found to be essential for insurmountable antagonism. To improve bioavailability of candesartan, chemical modification was examined to yield candesartan cilexetil, a prodrug of candesartan. Candesartan cilexetil is a potent and long-acting blocker that, when given once a day to patients, provides effective 24 hr blood pressure control.

MATERIALS
Product Number
Brand
Product Description

Candesartan cilexetil for peak identification, European Pharmacopoeia (EP) Reference Standard
Candesartan cilexetil for system suitability, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Candesartan cilexetil, ≥98% (HPLC)
Candesartan cilexetil, European Pharmacopoeia (EP) Reference Standard