Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.
Bioorg Med Chem Lett
; 18(6): 1926-30, 2008 Mar 15.
Article
in En
| MEDLINE
| ID: mdl-18308567
ABSTRACT
A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure-activity relationships are reported for these series. One potent orally bioavailable inhibitor had excellent PK properties and was active in a lung injury model in hyperoxia-exposed newborn rats.
Full text:
1
Database:
MEDLINE
Main subject:
Sulfonamides
/
Sulfonic Acids
/
Sulfonylurea Compounds
/
Carboxylic Acids
/
Receptors, Interleukin-8B
/
Lung
Limits:
Animals
/
Humans
Language:
En
Year:
2008
Type:
Article