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Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation

Authors
Park, Jin-Hun; Chang, Jeong-Soo; El-Gamal, Mohammed I.; Choi, Won-Kyoung; Lee, Woong San; Chung, Hye Jin; Kim, Hyun-Il; Cho, Young-Jin; Lee, Bong Sang; Jeon, Hong-Ryeol; Lee, Yong Sup; Choi, Young Wook; Lee, Jaehwi; Oh, Chang-Hyun
Issue Date
2010-10-01
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.20, no.19, pp.5895 - 5899
Abstract
Synthesis of novel amides and esters prodrugs of olmesartan is described. Their in vitro stability in rat plasma was tested. The results showed that the ester derivative IIa with n-octyl substituted dioxolone moiety was rapidly converted into olmesartan within 30 min. The pharmacokinetic parameters of IIa were studied and compared with those of olmesartan medoxomil. Compound IIa is proposed to be a promising prodrug of olmesartan. (C) 2010 Published by Elsevier Ltd.
Keywords
ANGIOTENSIN-CONVERTING ENZYME; II RECEPTOR ANTAGONISTS; BLOCKER; MEDOXOMIL; RENIN; ANGIOTENSIN-CONVERTING ENZYME; II RECEPTOR ANTAGONISTS; BLOCKER; MEDOXOMIL; RENIN; Antihypertensive; Olmesartan; Olmesartan medoxomil; Prodrug; Amide; Ester; Pharmacokinetics
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/131010
DOI
10.1016/j.bmcl.2010.07.089
Appears in Collections:
KIST Article > 2010
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