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Bioorg Med Chem Lett ; 21(22): 6693-8, 2011 Nov 15.
Article in English | MEDLINE | ID: mdl-21983444

ABSTRACT

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.


Subject(s)
11-beta-Hydroxysteroid Dehydrogenase Type 1/antagonists & inhibitors , 11-beta-Hydroxysteroid Dehydrogenase Type 1/metabolism , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Isoquinolines/chemistry , Isoquinolines/pharmacology , Animals , Cell Line , Diabetes Mellitus, Type 2/drug therapy , Enzyme Inhibitors/pharmacokinetics , Humans , Isoquinolines/pharmacokinetics , Mice , Mice, Inbred BALB C , Structure-Activity Relationship
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