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

✍ Scribed by Jin-Hun Park; 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

• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 560 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.07.089

✦ Synopsis

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.