Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers
<p>In the near future personalized medicine with nucleic acids will play a key role in molecular diagnostics and therapy, which require new properties of the nucleic acids, like stability against enzymatic degradation. Here we demonstrate that the replacement of nucleobases with PNA by functio...
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| Format: | Article |
| Language: | English |
| Published: |
Ivyspring International Publisher
2011-01-01
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| Series: | International Journal of Medical Sciences |
| Online Access: | http://www.medsci.org/v08p0387.htm |
| _version_ | 1818910863669592064 |
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| author | Ruediger Pipkorn, Manfred Wiessler, Waldemar Waldeck, Peter Lorenz, Ute Muehlhausen, Heinz Fleischhacker, Mario Koch, Klaus Braun |
| author_facet | Ruediger Pipkorn, Manfred Wiessler, Waldemar Waldeck, Peter Lorenz, Ute Muehlhausen, Heinz Fleischhacker, Mario Koch, Klaus Braun |
| author_sort | Ruediger Pipkorn, Manfred Wiessler, Waldemar Waldeck, Peter Lorenz, Ute Muehlhausen, Heinz Fleischhacker, Mario Koch, Klaus Braun |
| collection | DOAJ |
| description | <p>In the near future personalized medicine with nucleic acids will play a key role in molecular diagnostics and therapy, which require new properties of the nucleic acids, like stability against enzymatic degradation. Here we demonstrate that the replacement of nucleobases with PNA by functional molecules harbouring either a dienophile or a diene reactivity is feasible and confers all new options for functionalization. These newly developed derivatives allow independent multi-ligations of multi-faceted components by use of the inverse Diels Alder technology. The high chemical stability and the ease of synthesis qualify these polyamide building blocks as favourites for intracellular delivery and targeting applications. This allows local drug concentrations sufficient for imaging and therapy and simultaneously a reduction of the application doses. It is important to point out that this technology is not restricted to ligation of medicament material; it is also a candidate to develop new and highly efficient active compounds for a “sustainable pharmacy”.</p> |
| first_indexed | 2024-12-19T22:49:34Z |
| format | Article |
| id | doaj.art-9164442fc55c46d290110dac3387ae0f |
| institution | Directory Open Access Journal |
| issn | 1449-1907 |
| language | English |
| last_indexed | 2024-12-19T22:49:34Z |
| publishDate | 2011-01-01 |
| publisher | Ivyspring International Publisher |
| record_format | Article |
| series | International Journal of Medical Sciences |
| spelling | doaj.art-9164442fc55c46d290110dac3387ae0f2022-12-21T20:02:52ZengIvyspring International PublisherInternational Journal of Medical Sciences1449-19072011-01-0185387396Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based MonomersRuediger Pipkorn, Manfred Wiessler, Waldemar Waldeck, Peter Lorenz, Ute Muehlhausen, Heinz Fleischhacker, Mario Koch, Klaus Braun<p>In the near future personalized medicine with nucleic acids will play a key role in molecular diagnostics and therapy, which require new properties of the nucleic acids, like stability against enzymatic degradation. Here we demonstrate that the replacement of nucleobases with PNA by functional molecules harbouring either a dienophile or a diene reactivity is feasible and confers all new options for functionalization. These newly developed derivatives allow independent multi-ligations of multi-faceted components by use of the inverse Diels Alder technology. The high chemical stability and the ease of synthesis qualify these polyamide building blocks as favourites for intracellular delivery and targeting applications. This allows local drug concentrations sufficient for imaging and therapy and simultaneously a reduction of the application doses. It is important to point out that this technology is not restricted to ligation of medicament material; it is also a candidate to develop new and highly efficient active compounds for a “sustainable pharmacy”.</p>http://www.medsci.org/v08p0387.htm |
| spellingShingle | Ruediger Pipkorn, Manfred Wiessler, Waldemar Waldeck, Peter Lorenz, Ute Muehlhausen, Heinz Fleischhacker, Mario Koch, Klaus Braun Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers International Journal of Medical Sciences |
| title | Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers |
| title_full | Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers |
| title_fullStr | Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers |
| title_full_unstemmed | Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers |
| title_short | Enhancement of the Click Chemistry for the Inverse Diels Alder Technology by Functionalization of Amide-Based Monomers |
| title_sort | enhancement of the click chemistry for the inverse diels alder technology by functionalization of amide based monomers |
| url | http://www.medsci.org/v08p0387.htm |
| work_keys_str_mv | AT ruedigerpipkornmanfredwiesslerwaldemarwaldeckpeterlorenzutemuehlhausenheinzfleischhackermariokochklausbraun enhancementoftheclickchemistryfortheinversedielsaldertechnologybyfunctionalizationofamidebasedmonomers |