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

Compound IIa was found to be well absorbed from rat gastrointestinal tract and rapidly converted into olmesartan. After oral administration of IIa, the C max and AUC values of olmesartan were significantly greater than those observed after oral administration of olmesartan medoxomil. Compound IIa is...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 20; no. 19; pp. 5895 - 5899
Main Authors:	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
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 01-10-2010 Elsevier
Subjects:	Administration, Oral Amide Amides - chemistry Animals Antihypertensive Antihypertensive agents Biological and medical sciences Cardiovascular system Ester Esters General pharmacology Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacokinetics Male Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Olmesartan Olmesartan Medoxomil Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacokinetics Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions Pharmacology. Drug treatments Prodrug Prodrugs - chemical synthesis Prodrugs - chemistry Prodrugs - pharmacokinetics Rats Rats, Sprague-Dawley Tetrazoles - chemical synthesis Tetrazoles - chemistry Tetrazoles - pharmacokinetics Antihypertensive Ester Amide Olmesartan Prodrug Pharmacokinetics Olmesartan medoxomil Rat Rodentia Oral administration AT1 angiotensin receptor Metabolism Vertebrata Metabolic stability Mammalia Animal Antihypertensive agent Carboxamide Sartan derivatives Angiotensin antagonist Chemical synthesis
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