Literature DB >> 20728357

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

Jin-Hun Park1, Jeong-Soo Chang, Mohammed I El-Gamal, Won-Kyoung Choi, Woong San Lee, Hye Jin Chung, Hyun-Il Kim, Young-Jin Cho, Bong Sang Lee, Hong-Ryeol Jeon, Yong Sup Lee, Young Wook Choi, Jaehwi Lee, Chang-Hyun Oh.   

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.
Copyright © 2010. Published by Elsevier Ltd.

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Year:  2010        PMID: 20728357     DOI: 10.1016/j.bmcl.2010.07.089

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Product development studies on surface-adsorbed nanoemulsion of olmesartan medoxomil as a capsular dosage form.

Authors:  Sumita Singh; Kamla Pathak; Vikas Bali
Journal:  AAPS PharmSciTech       Date:  2012-09-11       Impact factor: 3.246

  1 in total

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