作为局部抗炎剂的取代吡唑并皮质类固醇。
Substituted pyrazolo corticoids as topical antiinflammatory agents.
作者信息
Hannah J, Kelly K, Patchett A A
出版信息
J Med Chem. 1975 Feb;18(2):168-72. doi: 10.1021/jm00236a012.
PMID:1120984
Abstract
The synthesis of a series of substituted pyrazolo corticoids is described. Of these 11beta,17alpha,21-trihydroxy-6,16alpha-dimethyl-4,6-pregnadieno[3,2-c]-2'-(4-pyridly)pyrazole (21) shows an excellent separation of systemic to local activity in the model animal test. Compound 21 exhibits high vasoconstriction activity in human volunteers and is clinically effective in the treatment of psoriasis.
摘要
描述了一系列取代吡唑并皮质激素的合成。其中，11β,17α,21-三羟基-6,16α-二甲基-4,6-孕二烯并[3,2-c]-2'-(4-吡啶基)吡唑（21）在模型动物试验中显示出全身活性与局部活性的出色分离。化合物21在人类志愿者中表现出高血管收缩活性，并且在银屑病治疗中具有临床疗效。
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