1.
Bioorg Med Chem Lett
; 18(12): 3632-7, 2008 Jun 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18495479
RESUMEN
An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replacement groups. Structure-based modeling provided the framework to efficiently effect this transformation and restore potencies to previous levels. This optimization removed a risk factor for potential idiosyncratic drug reactions.