Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10590800 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
Pyrrolopiperidinone acetic acids (PPAs) were identified as highly potent CRTh2 receptor antagonists. In addition, many of these compounds displayed slow-dissociation kinetics from the receptor. Structure-kinetic relationship (SKR) studies allowed optimisation of the kinetics to give potent analogues with long receptor residence half-lives of up to 23Â h. Low permeability was a general feature of this series, however oral bioavailability could be achieved through the use of ester prodrugs.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Miriam Andrés, Maria Antonia Buil, Marta Calbet, Oscar Casado, Jordi Castro, Paul R. Eastwood, Peter Eichhorn, Manel Ferrer, Pilar Forns, Imma Moreno, Silvia Petit, Richard S. Roberts,