1.
Bioorg Med Chem Lett
; 16(10): 2724-8, 2006 May 15.
Article
in English
| MEDLINE
| ID: mdl-16540318
ABSTRACT
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.
Subject(s)
Pyrimidines/pharmacology , Receptors, Interleukin-8B/antagonists & inhibitors , Administration, Oral , Animals , CHO Cells , Cricetinae , Humans , Microbial Sensitivity Tests , Pyrimidines/administration & dosage , Pyrimidines/pharmacokinetics , Recombinant Proteins/antagonists & inhibitors
2.
Bioorg Med Chem Lett
; 14(2): 545-8, 2004 Jan 19.
Article
in English
| MEDLINE
| ID: mdl-14698200
ABSTRACT
Structure-activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter type-2 inhibitors.
