1.
ACS Med Chem Lett
; 2(2): 102-6, 2011 Feb 10.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24900287
RESUMO
Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at 0.3 mg/kg, 14 significantly reduced blood lymphocyte counts 24 h postdose and attenuated a delayed type hypersensitivity (DTH) response to antigen challenge.
2.
Bioorg Med Chem Lett
; 18(18): 5023-6, 2008 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18755588
RESUMO
We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.