| Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan. | |
| | |
MedLine Citation:
|
PMID: 21641692 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
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. |
| | |
Authors:
|
Jeong-Soo Chang; Mohammed I El-Gamal; Woong San Lee; Hanan S Anbar; Hye Jin Chung; Hyun-Il Kim; Young-Jin Cho; Bong Sang Lee; Sun Ahe Lee; Ji Yun Moon; Dong Jin Lee; Hong-Ryeol Jeon; Jaehwi Lee; Young Wook Choi; Chang-Hyun Oh |
Publication Detail:
|
Type: JOURNAL ARTICLE Date: 2011-5-13 |
Journal Detail:
|
Title: European journal of medicinal chemistry Volume: - ISSN: 1768-3254 ISO Abbreviation: - Publication Date: 2011 May |
Date Detail:
|
Created Date: 2011-6-6 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: - |
Other Details:
|
Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
|
Copyright © 2011. Published by Elsevier Masson SAS. |
Affiliation:
|
College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156-756, Republic of Korea. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Distribution of primary care expenditure according to sex and age group: a retrospective analysis.
Next Document: Synthesis and cytotoxic activity of the heptaphylline and 7-methoxyheptaphylline series.