학술논문
1,7-Disubstituted oxyindoles are potent and selective EP3 receptor antagonists
Document Type
Article
Author
Source
Subject
*PROSTAGLANDIN antagonists
*INDOLE
*DRUG metabolism
*DERIVATIZATION
*LABORATORY rats
*PROSTANOIDS
*THERAPEUTICS
*
*
*
*
*
*
Language
ISSN
0960-894X
Abstract
Abstract: A series of novel 1,7-disubstituted oxyindoles were shown to be potent and selective EP3 receptor antagonists. Variation of substitution pattern at the C-3 position of indole enhanced in vitro metabolic stability of the resulting derivatives. Series 27a–c showed >1000-fold selectivity over a panel of prostanoid receptors including IP, FP, EP1, EP2 and EP4. These agents also featured low CYP inhibition and good activity in the functional rat platelet aggregation assay. [Copyright &y& Elsevier]