Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core
The development of new antibiotics with unique mechanisms of action is paramount to combating the growing threat of antibiotic resistance. Recently, based on inspiration from natural products, an asymmetrical polyacetylene core structure was examined for its bioactivity and found to have differentia...
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| Language: | English |
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MDPI AG
2024-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/29/24/5945 |
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| author | Tyler L. Skeen Rebekah L. Gresham Katherine A. Agamaite Olivia M. Molz Isabelle F. Westlake Sage M. Kregenow Al K. Romero Brian M. Flood Lauren E. Mazur Robert J. Hinkle Douglas D. Young |
| author_facet | Tyler L. Skeen Rebekah L. Gresham Katherine A. Agamaite Olivia M. Molz Isabelle F. Westlake Sage M. Kregenow Al K. Romero Brian M. Flood Lauren E. Mazur Robert J. Hinkle Douglas D. Young |
| author_sort | Tyler L. Skeen |
| collection | DOAJ |
| description | The development of new antibiotics with unique mechanisms of action is paramount to combating the growing threat of antibiotic resistance. Recently, based on inspiration from natural products, an asymmetrical polyacetylene core structure was examined for its bioactivity and found to have differential specificity for different bacterial species based on the substituents around the conjugated alkyne. This research further probes the structural requirements for bioactivity through a systematic synthesis and investigation of new compounds with variable carbon chain length, alkynyl subunits, and alcohol substitution. Furthermore, the research examines the activity of the new compounds towards the inhibition of biofilm formation. Overall, several key new polyyne compounds have been identified in both decreasing bacterial viability and in disrupting pre-formed biofilms. These properties are key in the fight against bacterial infections and will be helpful in the further development of new antibiotic agents. |
| format | Article |
| id | doaj-art-0214c84781a047cc8aebaf0949b7568d |
| institution | OA Journals |
| issn | 1420-3049 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-0214c84781a047cc8aebaf0949b7568d2025-08-20T02:01:20ZengMDPI AGMolecules1420-30492024-12-012924594510.3390/molecules29245945Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene CoreTyler L. Skeen0Rebekah L. Gresham1Katherine A. Agamaite2Olivia M. Molz3Isabelle F. Westlake4Sage M. Kregenow5Al K. Romero6Brian M. Flood7Lauren E. Mazur8Robert J. Hinkle9Douglas D. Young10Department of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USADepartment of Chemistry, William & Mary, Williamsburg, VA 23185, USAThe development of new antibiotics with unique mechanisms of action is paramount to combating the growing threat of antibiotic resistance. Recently, based on inspiration from natural products, an asymmetrical polyacetylene core structure was examined for its bioactivity and found to have differential specificity for different bacterial species based on the substituents around the conjugated alkyne. This research further probes the structural requirements for bioactivity through a systematic synthesis and investigation of new compounds with variable carbon chain length, alkynyl subunits, and alcohol substitution. Furthermore, the research examines the activity of the new compounds towards the inhibition of biofilm formation. Overall, several key new polyyne compounds have been identified in both decreasing bacterial viability and in disrupting pre-formed biofilms. These properties are key in the fight against bacterial infections and will be helpful in the further development of new antibiotic agents.https://www.mdpi.com/1420-3049/29/24/5945antibioticsalkynesbiofilmsstructure–activity relationshipsGlaser–Hay reaction |
| spellingShingle | Tyler L. Skeen Rebekah L. Gresham Katherine A. Agamaite Olivia M. Molz Isabelle F. Westlake Sage M. Kregenow Al K. Romero Brian M. Flood Lauren E. Mazur Robert J. Hinkle Douglas D. Young Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core Molecules antibiotics alkynes biofilms structure–activity relationships Glaser–Hay reaction |
| title | Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core |
| title_full | Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core |
| title_fullStr | Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core |
| title_full_unstemmed | Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core |
| title_short | Elucidation of Antimicrobials and Biofilm Inhibitors Derived from a Polyacetylene Core |
| title_sort | elucidation of antimicrobials and biofilm inhibitors derived from a polyacetylene core |
| topic | antibiotics alkynes biofilms structure–activity relationships Glaser–Hay reaction |
| url | https://www.mdpi.com/1420-3049/29/24/5945 |
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