Iso-Partricin, an Aromatic Analogue of Amphotericin B: How Shining Light on Old Drugs Might Help Create New Ones
Partricin is a heptaene macrolide antibiotic complex that exhibits exceptional antifungal activity, yet poor selective toxicity, in the pathogen/host system. It consists of two compounds, namely partricin A and B, and both of these molecules incorporate two <i>cis</i>-type bonds within t...
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MDPI AG,
2021-09-01T00:00:00Z.
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| Achoimre: | Partricin is a heptaene macrolide antibiotic complex that exhibits exceptional antifungal activity, yet poor selective toxicity, in the pathogen/host system. It consists of two compounds, namely partricin A and B, and both of these molecules incorporate two <i>cis</i>-type bonds within their heptaenic chromophores: 28<i>Z</i> and 30<i>Z</i>. In this contribution, we have proven that partricins are susceptible to a chromophore-straightening photoisomerization process. The occurring 28<i>Z</i>→28<i>E</i> and 30<i>Z</i>→30<i>E</i> switches are irreversible in given conditions, and they are the only structural changes observed during the experiment. The obtained <i>all-trans</i> partricin's derivatives, namely iso-partricins A and B, exhibit very promising features, potentially resulting in the improvement of their selective toxicity. |
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| Cur síos ar an mír: | 10.3390/antibiotics10091102 2079-6382 |