Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: the role of a hydrogen-bond acceptor in long receptor residence times.
Bioorg Med Chem Lett
; 24(21): 5127-33, 2014 Nov 01.
Article
in En
| MEDLINE
| ID: mdl-25437506
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Bridged Bicyclo Compounds
/
Receptors, Prostaglandin
/
Receptors, Immunologic
/
Acetates
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2014
Document type:
Article
Affiliation country:
Spain