Synthesis of novel ceramide-like penetration enhancers

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• 作者：Má ; ria Taká ; cs^a ; Má ; té ; Bubenyá ; k^a ; ^{bmate@gyok.sote.hu} ; Andrá ; s Vá ; radi^a ; Balá ; zs Blazics^b ; Pé ; ter Horvá ; th^a ; Jó ; zsef K&#xf6 ; k&#xf6 ; si^a
• 关键词：Ceramide ; Isostere replacement ; Penetration enhancer ; Oxime
• 刊名：Tetrahedron Letters
• 出版年：2011
• 出版时间：20 April 2011
• 年：2011
• 卷：52
• 期：16
• 页码：1863-1865
• 全文大小：375 K

文摘

Ceramide-like penetration enhancers have been synthesized by isosteric replacements of the 1-hydroxymethyl and amide moieties of natural ceramides. Metabolically more stable oxime and five-membered heterocyclic (1,2,4-oxadiazole, 1,2,4-triazole, tetrazole) analogues are more polar and possess H-bond acceptor properties, which make them potentially useful in optimizing key intermolecular features in interactions between the modified ceramide structures and the lipid layers of stratum corneum.