Synthesis and transdermal permeation-enhancing activity of carbonate and carbamate analogs of Transkarbam 12
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
16942882
DOI
10.1016/j.bmc.2006.08.014
PII: S0968-0896(06)00675-4
Knihovny.cz E-resources
- MeSH
- Adjuvants, Pharmaceutic chemical synthesis pharmacokinetics MeSH
- Esters MeSH
- Carbamates chemistry pharmacokinetics MeSH
- Skin Absorption drug effects MeSH
- Permeability MeSH
- Swine MeSH
- Carbonates * MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Adjuvants, Pharmaceutic MeSH
- Esters MeSH
- Carbamates MeSH
- transkarbam 12 MeSH Browser
- Carbonates * MeSH
Transkarbam 12 (5-(dodecyloxycarbonyl)pentylammonium-5-(dodecyloxycarbonyl)pentylcarbamate, T12) is a highly effective skin permeation enhancer. In this study, ester groups in the molecule of T12 were replaced by carbonate and carbamate ones, respectively. The in vitro permeation-enhancing activities were evaluated using porcine skin and compared with those of T12 and previously prepared series of amide, ketone, and alkyl analogs. According to the activities and behavior of the compounds in donor samples, ester group is essential for the activity of T12; its replacement not only decreases the enhancing potency, but is likely to change the mechanism of action.
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