El-Gamal, Mohammed I. Anbar, Hanan S. Chung, Hye Jin Kim, Hyun-Il Cho, Young-Jin Lee, Bong Sang Lee, Sun Ahe Moon, Ji Yun Lee, Dong Jin Kwon, Dow Choi, Won-Jai Jeon, Hong-Ryeol Oh, Chang-Hyun 2024-01-20T12:34:38Z 2024-01-20T12:34:38Z 2022-01-10 2013-03-01 0960-894X https://pubs.kist.re.kr/handle/201004/128254 Synthesis of a new ester prodrug of olmesartan, olmesartan hexetil (1), is described. It is in vitro stabilities and in vivo pharmacokinetics (PK) were evaluated. It showed high stability in simulated gastric juice, and was rapidly hydrolyzed to olmesartan in rat liver microsomes and rat plasma in vitro. C-max and AUC(last) for olmesartan were significantly increased in case of hexetil prodrug, compared with olmesartan medoxomil. Olmesartan hexetil is proposed to be an efficient prodrug of olmesartan with markedly increased oral bioavailability. (C) 2013 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. II RECEPTOR ANTAGONISTS ANGIOTENSIN-CONVERTING ENZYME BIOACTIVATING HYDROLASE MEDOXOMIL BLOCKER RENIN ACIDS Discovery of olmesartan hexetil: A new potential prodrug of olmesartan Article 10.1016/j.bmcl.2012.12.090 1 Bioorganic & Medicinal Chemistry Letters, v.23, no.5, pp.1347 - 1350 Bioorganic & Medicinal Chemistry Letters 23 5 1347 1350 scie scopus 000314693400039 2-s2.0-84873714069 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article II RECEPTOR ANTAGONISTS ANGIOTENSIN-CONVERTING ENZYME BIOACTIVATING HYDROLASE MEDOXOMIL BLOCKER RENIN ACIDS Antihypertensive Olmesartan medoxomil Olmesartan hexetil Prodrug Ester Pharmacokinetics