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

Year: 2024

Type: article

Abstract: Tetramic acid-containing natural products are well known for their promising biological activity against various diseases. In our previous study, we reported fungal-derived tetramic acid-containing natural products with activity against Trichomonas vaginalis . Here, we demonstrate that Mycoplasma genitalium is also highly susceptible to this chemotype and we uncovered the initial structure activity relationships on disparate tetramate chemotypes in phomasetin ( 6 ) and pyrrolocin A ( 10 ). Further, 6 and 10 were modified using “click” chemistry to re-engineer bioactivity. Compounds 6 and 10 hold promise as a pipeline-diversifying chemotype for promising leads against T . vaginalis and M . genitalium .

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.4c00386