Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.
Bioorg Med Chem Lett
; 23(24): 6640-4, 2013 Dec 15.
Article
in En
| MEDLINE
| ID: mdl-24215891
ABSTRACT
A class of α-methyltryptamine sulfonamide glucocorticoid receptor (GR) modulators was optimized for agonist activity. The design of ligands was aided by molecular modeling, and key function-regulating pharmacophoric points were identified that are critical in achieving the desired agonist effect in cell based assays. Compound 27 was profiled in vitro and in vivo in models of inflammation. Analogs could be rapidly prepared in a parallel approach from aziridine building blocks.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Sulfonamides
/
Receptors, Glucocorticoid
/
Tryptamines
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2013
Document type:
Article