Author: Reidl, Cory T.; Heath, Tahirah K.; Darwish, Iman; Torrez, Rachel M.; Moore, Maxwell; Gild, Elliot; Nocek, Boguslaw P.; Starus, Anna; Holz, Richard C.; Becker, Daniel P.
Title: Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE Cord-id: io0qflt2 Document date: 2020_9_11
ID: io0qflt2
Snippet: 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 th
Document: 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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