Semisynthetic Tetramate-Containing Fungal Metabolites\nwith Activity against <i>Trichomonas vaginalis</i> and <i>Mycoplasma genitalium</i>

Tetramic\nacid-containing natural products are well known for their\npromising biological activity against various diseases. In our previous\nstudy, we reported fungal-derived tetramic acid-containing natural\nproducts with activity against <i>Trichomonas vaginalis</i>. Here, we demonstrate that <i>Mycoplasma genitalium</i> is also highly susceptible to this chemotype and we uncovered the\ninitial structure activity relationships on disparate tetramate chemotypes\nin phomasetin (<b>6</b>) and pyrrolocin A (<b>10</b>).\nFurther, <b>6</b> and <b>10</b> were modified using “click”\nchemistry to re-engineer bioactivity. Compounds <b>6</b> and <b>10</b> hold promise as a pipeline-diversifying chemotype for promising\nleads against <i>T</i>. <i>vaginalis</i> and <i>M</i>. <i>genitalium</i>.

Publication Details

Journal
Figshare
Published
2024-10-24
DOI
https://doi.org/10.1021/acsmedchemlett.4c00386.s001
Primary Topic
Reproductive tract infections research
Type
article
Field-Weighted Citation Impact
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article

Semisynthetic Tetramate-Containing Fungal Metabolites\nwith Activity against Trichomonas vaginalis and Mycoplasma genitalium

Figshare
Reproductive tract infections research
article

Semisynthetic Tetramate-Containing Fungal Metabolites\nwith Activity against Trichomonas vaginalis and Mycoplasma genitalium

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Abstract

Tetramic\nacid-containing natural products are well known for their\npromising biological activity against various diseases. In our previous\nstudy, we reported fungal-derived tetramic acid-containing natural\nproducts with activity against <i>Trichomonas vaginalis</i>. Here, we demonstrate that <i>Mycoplasma genitalium</i> is also highly susceptible to this chemotype and we uncovered the\ninitial structure activity relationships on disparate tetramate chemotypes\nin phomasetin (<b>6</b>) and pyrrolocin A (<b>10</b>).\nFurther, <b>6</b> and <b>10</b> were modified using “click”\nchemistry to re-engineer bioactivity. Compounds <b>6</b> and <b>10</b> hold promise as a pipeline-diversifying chemotype for promising\nleads against <i>T</i>. <i>vaginalis</i> and <i>M</i>. <i>genitalium</i>.

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Openalex Percentile: Top 69%
Reproductive tract infections research
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