Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 24, Pages 7720-7725Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.08.052
Keywords
prostacyclin; IP receptor agonist; N-acylsulfonamide; N-acylsulfonylurea; prodrug
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N-Acylsulfonamide and N-acylsulfonylurea derivatives of the carboxylic acid prostacyclin receptor agonist 1 were synthesized and their potential as prodrug forms of the carboxylic acid was evaluated in vitro and in vivo. These compounds were converted to the active compound 1 by hepatic microsomes from rats, dogs, monkeys, and humans, and some of the compounds were shown to yield sustained plasma concentrations of 1 when they were orally administered to monkeys. These types of analogues, including NS-304 (2a), are potentially useful prodrugs of 1. (c) 2007 Elsevier Ltd. All rights reserved.
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