Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan
- Authors
- Chang, Jeong-Soo; El-Gamal, Mohammed I.; Lee, Woong San; Anbar, Hanan S.; Chung, Hye Jin; Kim, Hyun-Il; Cho, Young-Jin; Lee, Bong Sang; Lee, Sun Ahe; Moon, Ji Yun; Lee, Dong Jin; Jeon, Hong-Ryeol; Lee, Jaehwi; Choi, Young Wook; Oh, Chang-Hyun
- Issue Date
- Sep-2011
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- Antihypertensive; Olmesartan; Olmesartan medoxomil; Prodrug; Ester; Pharmacokinetics
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.9, pp 3564 - 3569
- Pages
- 6
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 46
- Number
- 9
- Start Page
- 3564
- End Page
- 3569
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/21313
- DOI
- 10.1016/j.ejmech.2011.05.019
- ISSN
- 0223-5234
1768-3254
- 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, C-max and AUC(last) 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. (C) 2011 Elsevier Masson SAS. All rights reserved.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - College of Pharmacy > School of Pharmacy > 1. Journal Articles
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/21313)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.