Aza-beta3-cyclotetrapeptides |
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Authors: | Salaün Arnaud Mocquet Clémence Perochon Romain Lecorgne Aurélien Le Grel Barbara Potel Michel Le Grel Philippe |
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Affiliation: | ICMV, UMR CNRS 6226, Université de Rennes I, 263 avenue du Général Leclerc, 35042 Rennes, Cedex, France. |
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Abstract: | The cyclization of aza-beta(3)-tetrapeptides gives access to new CTP (cyclotetrapeptide) analogues. These stereocontrolled templates are assembled without any asymmetric synthesis. X-ray crystallographic structure and NMR analysis show that the macrocyclic scaffold is characterized by a fully cooperative intramolecular H-bond network, in sharp contrast with the nanotubular assemblies observed for beta(3)-cyclotetrapeptides. This folding property reduces considerably the polarity of aza-beta(3)-tetrapeptides and should be useful in addressing intracellular targets. |
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