Truncated S-MGBs : towards a parasite-specific and low aggregation chemotype
This journal is © The Royal Society of Chemistry..
This paper describes the design and synthesis of Strathclyde minor groove binders (S-MGBs) that have been truncated by the removal of a pyrrole ring in order to mimic the structure of the natural product, disgocidine. S-MGBs have been found to be active against many different organisms, however, selective antiparasitic activity is required. A panel of seven truncated S-MGBs was prepared and the activities examined against a number of clinically relevant organisms including several bacteria and parasites. The effect of the truncation strategy on S-MGB aggregation in aqueous environment was also investigated using 1H inspection and DOSY experiments. A lead compound, a truncated S-MGB, which possesses significant activity only against trypanosomes and Leishmania has been identified for further study and was also found to be less affected by aggregation compared to its full-length analogue.
| Errataetall: |
ErratumIn: RSC Med Chem. 2021 Nov 26;12(12):2071. - PMID 35024615 |
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| Medienart: |
E-Artikel |
| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
RSC medicinal chemistry - 12(2021), 8 vom: 18. Aug., Seite 1391-1401 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Brooke, Daniel P [VerfasserIn] |
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Date Revised 22.03.2023 published: Electronic-eCollection ErratumIn: RSC Med Chem. 2021 Nov 26;12(12):2071. - PMID 35024615 Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1039/d1md00110h |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM329907905 |
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| 500 | |a ErratumIn: RSC Med Chem. 2021 Nov 26;12(12):2071. - PMID 35024615 | ||
| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a This journal is © The Royal Society of Chemistry. | ||
| 520 | |a This paper describes the design and synthesis of Strathclyde minor groove binders (S-MGBs) that have been truncated by the removal of a pyrrole ring in order to mimic the structure of the natural product, disgocidine. S-MGBs have been found to be active against many different organisms, however, selective antiparasitic activity is required. A panel of seven truncated S-MGBs was prepared and the activities examined against a number of clinically relevant organisms including several bacteria and parasites. The effect of the truncation strategy on S-MGB aggregation in aqueous environment was also investigated using 1H inspection and DOSY experiments. A lead compound, a truncated S-MGB, which possesses significant activity only against trypanosomes and Leishmania has been identified for further study and was also found to be less affected by aggregation compared to its full-length analogue | ||
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| 700 | 1 | |a McGee, Leah M C |e verfasserin |4 aut | |
| 700 | 1 | |a Giordani, Federica |e verfasserin |4 aut | |
| 700 | 1 | |a Cross, Jasmine M |e verfasserin |4 aut | |
| 700 | 1 | |a Khalaf, Abedawn I |e verfasserin |4 aut | |
| 700 | 1 | |a Irving, Craig |e verfasserin |4 aut | |
| 700 | 1 | |a Gillingwater, Kirsten |e verfasserin |4 aut | |
| 700 | 1 | |a Shaw, Craig D |e verfasserin |4 aut | |
| 700 | 1 | |a Carter, Katharine C |e verfasserin |4 aut | |
| 700 | 1 | |a Barrett, Michael P |e verfasserin |4 aut | |
| 700 | 1 | |a Suckling, Colin J |e verfasserin |4 aut | |
| 700 | 1 | |a Scott, Fraser J |e verfasserin |4 aut | |
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