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 2024-01-20T18:31:19Z 2024-01-20T18:31:19Z 2022-01-10 2010-10-01 0960-894X https://pubs.kist.re.kr/handle/201004/131010 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. English Pergamon Press Ltd. ANGIOTENSIN-CONVERTING ENZYME II RECEPTOR ANTAGONISTS BLOCKER MEDOXOMIL RENIN Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation Article 10.1016/j.bmcl.2010.07.089 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.19, pp.5895 - 5899 Bioorganic & Medicinal Chemistry Letters 20 19 5895 5899 scie scopus 000281735600064 2-s2.0-77957561249 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article ANGIOTENSIN-CONVERTING ENZYME II RECEPTOR ANTAGONISTS BLOCKER MEDOXOMIL RENIN Antihypertensive Olmesartan Olmesartan medoxomil Prodrug Amide Ester Pharmacokinetics