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Bioorg Med Chem Lett
; 21(22): 6693-8, 2011 Nov 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21983444
RESUMEN
Derived from the HTS hit 1, a series of hydroxyisoquinolines was discovered as potent and selective 11ß-HSD1 inhibitors with good cross species activity. Optimization of substituents at the 1 and 4 positions of the isoquinoline group in addition to the core modifications, with a special focus on enhancing metabolic stability and aqueous solubility, resulted in the identification of several compounds as potent advanced leads.