The synthesis and antiinflammatory activities of new steroidal 20-carboxamides, (20R)- and (20S)-21-(N-substituted amino)-11 beta,17,20-trihydroxy-3,21-dioxo-1,4-pregnadiene are described. These compounds were prepared from the respective isomer of 20-dihydroprednisolonic acid, (20R)- and (20S)-11 beta,17,20-trihydroxy-3-oxo-1,4-pregnadien-21-oic acid, by coupling with primary amines after the activation
新型甾体20-羧酰胺,(20R)-和(20S)-21-(N-取代的
氨基)-11β,17,20-三羟基-3,21-二氧代-1,4-孕烷二烯的合成及抗炎活性描述。这些化合物是由20-二氢
泼尼松酸的相应异构体(20R)-和(20S)-11β,17,20-三羟基-3-氧代-1,4-孕烯基-21-oic酸与N,N1-二环己基碳二
亚胺(
DCC)和
1-羟基苯并三唑活化甾体酸后的
伯胺 通过还原甲基(20R)-和(20S)-11 beta,17,20-三羟基-3-氧代-1,4-孕烷-21-甲基来实现20-甲酰胺在C-20的构型分配的确认。 (20R)-和(20S)-11 beta,17,20,21-tetrahydroxy-3-oxo-1在C-20的已知立体
化学 4-
孕烯二酮通过
巴豆油诱导的耳部
水肿试验评估了这些甾体20-羧酰胺的局部抗炎活性,并通过棉球颗粒肉芽肿
生物试验评估了它们的局部和全身抗炎活性。这些