Oligocarbamate molecular transporters: design, synthesis, and biological evaluation of a new class of transporters for drug delivery.

作者: Paul A. Wender , Jonathan B. Rothbard , Theodore C. Jessop , Erik L. Kreider , Bryan L. Wylie

DOI: 10.1021/JA0275109

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摘要: Molecular transporters have the ability to deliver drugs and probe molecules into cells tissues irrespective of their physical properties. We now report design, synthesis, biological evaluation a new family molecular transporters, guanidinylated oligocarbamates that enable exceptionally efficient uptake tissues. The synthesis features solid-phase stepwise oligomerization obtain single step perguanidinylation for facile introduction up nine guanidinium groups. oligocarbamate 9-mer is found be among most known, entering faster than even d-Arg9 HIV-1 Tat49-57. Significantly, this also enables formidable skin barrier molecule by itself does not penetrate skin.

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