Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists
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Add time:08/24/2019 Source:sciencedirect.com
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 23 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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