Discovery of olmesartan hexetil: A new potential prodrug of olmesartan
- Discovery of olmesartan hexetil: A new potential prodrug of olmesartan
- 모하메드엘가말; Hanan S. Anbar; 정혜진; 김현일; 조영진; 이봉상; 이선애; 문지윤; 이동진; 권도우; 최원재; 전홍렬; 오창현
- Antihypertensive; Ester; Olmesartan medoxomil; Pharmacokinetics; Olmesartan hexetil; Prodrug
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 23, NO 5, 1347-1350
- Synthesis of a new ester prodrug of olmesartan, olmesartan hexetil (1), is described. It is in vitro stabilities and in vivo pharmacokinetics (PK) were evaluated. It showed high stability in simulated gastric juice, and was rapidly hydrolyzed to olmesartan in rat liver microsomes and rat plasma in vitro. Cmax and AUClast for olmesartan were significantly increased in case of hexetil prodrug, compared with olmesartan medoxomil. Olmesartan hexetil is proposed to be an efficient prodrug of olmesartan with markedly increased oral bioavailability
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