Soft β-adrenergic agonists for the topical treatment of psoriasis

HS Gill, S Freeman, WJ Irwin, KA Wilson

文献索引：Gill; Freeman; Irwin; Wilson European Journal of Medicinal Chemistry, 1996 , vol. 31, # 11 p. 847 - 859

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被引用次数: 5

摘要

The soft-drug 1 (R= Me, Et) and pro-soft-drug 3 have been prepared as models of topical anti-psoriatic β-adrenergic agonists. The chemical hydrolysis of 3 proceeded via the acid 18 with a maximum stability at apparent pH∼ 4.0. In the presence of PLCE, the required metabolism of 3 to the soft-drug 1 (R= Et) was achieved, which slowly degraded to the dihydroxy acid 2. Soft-drug 1 (R= Et) was poorly transported across a silicone membrane, ...