Chang, Jeong-Soo El-Gamal, Mohammed I. Lee, Woong San Anbar, Hanan S. Chung, Hye Jin Kim, Hyun-Il Cho, Young-Jin Lee, Bong Sang Lee, Sun Ahe Moon, Ji Yun Lee, Dong Jin Jeon, Hong-Ryeol Lee, Jaehwi Choi, Young Wook Oh, Chang-Hyun 2024-01-20T16:30:47Z 2024-01-20T16:30:47Z 2022-01-10 2011-09 0223-5234 https://pubs.kist.re.kr/handle/201004/130006 Synthesis of new ester prodrugs of olmesartan is described. Their in vitro stabilities in simulated gastric juice, rat plasma, and rat liver microsomes were tested. And the pharmacokinetic parameters for olmesartan after their oral administration were also estimated and compared with those in case of olmesartan medoxomil. Compounds 13 and 14 demonstrated high stability in simulated gastric juice and were rapidly metabolized to olmesartan in rat liver microsomes and rat plasma in vitro. In addition, C-max and AUC(last) parameters were significantly increased in case of compounds 13 and 14 compared with olmesartan medoxomil. These results indicate that compounds 13 and 14 with cyclohexylcarboxyethyl and adamantylcarboxymethyl promoieties, respectively, are promising prodrugs of olmesartan with markedly increased oral bioavailability. (C) 2011 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER ANGIOTENSIN-CONVERTING ENZYME II RECEPTOR ANTAGONISTS BLOCKER MEDOXOMIL RENIN Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan Article 10.1016/j.ejmech.2011.05.019 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.9, pp.3564 - 3569 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46 9 3564 3569 scie scopus 000295237400003 2-s2.0-80052942627 Chemistry, Medicinal Pharmacology & Pharmacy Article ANGIOTENSIN-CONVERTING ENZYME II RECEPTOR ANTAGONISTS BLOCKER MEDOXOMIL RENIN Antihypertensive Olmesartan Olmesartan medoxomil Prodrug Ester Pharmacokinetics