Author/Authors :
Xiangdong Su، نويسنده , , Harshani Lawrence، نويسنده , , Dharshini Ganeshapillai، نويسنده , , Adrian Cruttenden، نويسنده , , Atul Purohit، نويسنده , , Michael J Reed، نويسنده , , Nigel Vicker، نويسنده , , Barry VL Potter، نويسنده ,
Abstract :
Extensive structural modifications to the 18β-glycyrrhetinic acid template are described and their effects on the SAR of the 11β-hydroxysteroid dehydrogenase isozymes type 1 and 2 from the rat are investigated. Isoform selective inhibitors have been discovered and compound 7 N-(2-hydroxyethyl)-3β-hydroxy-11-oxo-18β-olean-12-en-30-oic acid amide is highlighted as a very potent selective inhibitor of 11β-hydroxysteroid dehydrogenase 2 with an IC50 = 4 pM.
