作者: Paul A. Wender , Jonathan B. Rothbard , Theodore C. Jessop , Erik L. Kreider , Bryan L. Wylie
DOI: 10.1021/JA0275109
关键词:
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.