A series of novel N-arylsulfonylated C-homoaporphine alkaloids were synthesized under microwave irradiation and evaluated for their antiplatelet and antimicrobial activities. Among the series, compounds , , , , , , , , and demonstrated highly potent (∼3-fold) platelet aggregation inhibitory activity than acetylsalicylic acid (IC = 21.34 μg/mL). Several N-arylsulfonylated C-homoaporphines also exhibited promising antimicrobial activity against various strains, including , , and , with minimum inhibitory concentrations (MIC) of 12.5, 6.25, and 12.5 μg/mL, respectively, comparable to Ketoconazole [MIC = 12.5 μg/mL (MP and AN strain); 6.25 μg/mL (TR strain)]. showed potent antibacterial activity (IC = 6.25 μg/mL against and ) compared to Ampicillin (IC = 12.5 μg/mL). After thorough structure-activity relationship (SAR) and studies, C-homoaporphines were identified as a novel class of antiplatelet and antimicrobial agents.
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| http://dx.doi.org/10.1021/acsmedchemlett.4c00491 | DOI Listing |
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