Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10590804 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
The correct positioning and orientation of an hydrogen bond acceptor (HBA) in the tail portion of the biaryl series of CRTh2 antagonists is a requirement for long receptor residence time. The HBA in combination with a small steric substituent in the core section (Rcore â  H) gives access to compounds with dissociation half-lives of ⩾24 h.
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Authors
Juan Antonio Alonso, Miriam Andrés, Mónica Bravo, Maria Antonia Buil, Marta Calbet, Jordi Castro, Paul R. Eastwood, Cristina Esteve, Manel Ferrer, Pilar Forns, Elena Gómez, Jacob González, Estrella Lozoya, Marta Mir, Imma Moreno, Silvia Petit,