Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan
- Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan
- 장정수; 엘가말; 이웅산; Hanan S. Anbar; 정혜진; 김현일; 조영진; 이봉상; 이선애; 문지연; 이동진; 전홍렬; 이재희; 최영욱; 오창현
- Antihypertensive; Olmesartan medoxomil; Prodrug; Olmesartan; Ester; Pharmacokinetics
- Issue Date
- European journal of medicinal chemistry
- VOL 46, NO 9, 3564-3569
- Synthesis of new ester prodrugs of olmesartan is described. Their in vitro stabilities in simulated gastric
juice, rat plasma, and rat liver microsomes were tested. And the pharmacokinetic parameters for
olmesartan after their oral administration were also estimated and compared with those in case of
olmesartan medoxomil. Compounds 13 and 14 demonstrated high stability in simulated gastric juice and
were rapidly metabolized to olmesartan in rat liver microsomes and rat plasma in vitro. In addition, Cmax
and AUClast parameters were significantly increased in case of compounds 13 and 14 compared with
olmesartan medoxomil. These results indicate that compounds 13 and 14 with cyclohexylcarboxyethyl
and adamantylcarboxymethyl promoieties, respectively, are promising prodrugs of olmesartan with
markedly increased oral bioavailability.
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