Structure-based design of 7-azaindole-pyrrolidine amides as inhibitors of 11β-hydroxysteroid dehydrogenase type I

Structure-based optimisation of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)-directed high-throughput screening hit led to 7-azaindole-derivatives displaying single digit nanomolar IC50, selective against 11β-HSD2 and exhibiting good inhibition of 11β-HSD1 (IC50 < 1 μM) in 3T3L1 adipocytes.