title: Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation.
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.
authors: Biomaterials Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
authors: Jin-Hun
authors: JH
authors: Park
authors: Jeong-Soo
authors: JS
authors: Chang
authors: Mohammed I
authors: MI
authors: El-Gamal
authors: Won-Kyoung
authors: WK
authors: Choi
authors: Woong San
authors: WS
authors: Lee
authors: Hye Jin
authors: HJ
authors: Chung
authors: Hyun-Il
authors: HI
authors: Kim
authors: Young-Jin
authors: YJ
authors: Cho
authors: Bong Sang
authors: BS
authors: Lee
authors: Hong-Ryeol
authors: HR
authors: Jeon
authors: Yong Sup
authors: YS
authors: Lee
authors: Young Wook
authors: YW
authors: Choi
authors: Jaehwi
authors: J
authors: Lee
authors: Chang-Hyun
authors: CH
authors: Oh
mesh_terms: D000284:Administration, Oral; D000577:Amides / Q000737:chemistry*; D000818:Animals; D004952:Esters; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D000068557:Olmesartan Medoxomil; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D000577:Amides; D004952:Esters; D007093:Imidazoles; D011355:Prodrugs; D013777:Tetrazoles; D000068557:Olmesartan Medoxomil; C437965:olmesartan