Publication | Open Access
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin
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2018
Year
Combinatorial ChemistryBioorganic ChemistryOrganic ChemistryPharmaceutical ChemistryChemical DerivativeMedicinal ChemistryDiversity Oriented SynthesisBiological EvaluationPtm StructureHydrazide DerivativesAntimicrobial Drug DiscoveryDozen OximeBiochemistryDiversity-oriented SynthesisAntimicrobial CompoundNatural Product SynthesisPharmacologyTerpene ScaffoldNatural SciencesMedicineDerivative (Chemistry)Drug DiscoveryDrug Analysis
A dozen oxime, hydrazine and hydrazide derivatives of platensimycin (PTM) analogues were synthesized, some of which showed strong antibacterial activities and were shown to be stable under the bioassay conditions. Docking analysis revealed that they have certain new interactions with β-ketoacyl-[acyl carrier protein] synthase II (FabF), suggesting that Schiff base formation on its terpene scaffold is an effective strategy to diversify PTM structure.
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