Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan

Title
Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan
Authors
장정수엘가말이웅산Hanan S. Anbar정혜진김현일조영진이봉상이선애문지연이동진전홍렬이재희최영욱오창현
Keywords
Antihypertensive; Olmesartan medoxomil; Prodrug; Olmesartan; Ester; Pharmacokinetics
Issue Date
2011-09
Publisher
European journal of medicinal chemistry
Citation
VOL 46, NO 9, 3564-3569
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/40683
ISSN
0223-5234
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KIST Publication > Article
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