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Inhibitors of the bacterial enzyme dapE-encoded N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE; EC 3.5.1.18) hold promise as antibiotics with a new mechanism of action. Herein we describe the discovery of a new series of indoline sulfonamide DapE inhibitors from a high-throughput screen and the synthesis of a series of analogs. Inhibitory potency was measured by a ninhydrin-based DapE assay recently developed by our group. Molecular docking experiments suggest active site binding with the sulfonamide acting as a zinc-binding group (ZBG).
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10.3390/antibiotics9090595
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document_parses/pdf_json/8abddf5dd40450d7b94d617cccf0e3413b3cc833.json
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document_parses/pmc_json/PMC7560015.xml.json
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Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE
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