Journal of Enzyme Inhibition and Medicinal Chemistry · 2017 · 62 citations · 12 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryStructure-activity RelationshipsAntibacterial PharmacologyAntibiotic ResistanceAntifungal AgentsChemical Library DesignStructure-activity Relationship AnalysisFungal Drug ResistanceMycobacterium Tuberculosis InfectionNew Antifungal AgentsNovel Antibacterial AgentsNovel Antibacterial Drug DiscoveryStructure - Activity Relationship OptimizationTuberculosis Drug Development
values of ≤16,760. Compounds derived from trimethoxy substituent scaffolds with monofluoro substitution on the B ring of the chalcone structure exhibited superior inhibition activity compared to corresponding hydroxy analogs. In terms of antimicrobial activity, most compounds (3, 9, 12-14, and 23) exhibited moderate to potent activity against the bacteria, and the antifungal activities of compounds 3, 13, 15, 20, and 22 were comparable to those of reference drugs ampicillin and fluconazole.
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