1.
Bioorg Med Chem Lett
; 18(6): 2032-7, 2008 Mar 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18304812
RESUMO
The discovery, synthesis and in vitro activity of a novel series of rhodanine based phosphodiesterase-4 (PDE4) inhibitors is described. Structure-activity relationship studies directed toward improving potency led to the development of submicromolar inhibitors 2n and 3i (IC(50)=0.89 & 0.74 microM). The replacement of rhodanine with structurally related heterocycles was also investigated and led to the synthesis of pseudothiohydantoin 7 (IC(50)=0.31 microM).