| Literature DB >> 25437506 |
Juan Antonio Alonso1, Miriam Andrés1, Mónica Bravo1, Maria Antonia Buil1, Marta Calbet1, Jordi Castro1, Paul R Eastwood1, Cristina Esteve1, Manel Ferrer1, Pilar Forns2, Elena Gómez1, Jacob González1, Estrella Lozoya1, Marta Mir1, Imma Moreno1, Silvia Petit1, Richard S Roberts3, Sara Sevilla1, Bernat Vidal1, Laura Vidal1, Pere Vilaseca1.
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 (R(core) ≠ H) gives access to compounds with dissociation half-lives of ⩾ 24h.Entities:
Keywords: CRTh2 antagonist; Hydrogen bond acceptor; Long residence time; Structure–activity relationship (SAR); Structure–kinetic relationship (SKR)
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Year: 2014 PMID： 25437506 DOI： 10.1016/j.bmcl.2014.08.028
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823