Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE
- Loyola Univ., Chicago, IL (United States); Northwestern Univ., Evanston, IL (United States)
- Loyola Univ., Chicago, IL (United States)
- Argonne National Lab. (ANL), Argonne, IL (United States)
- Colorado School of Mines, Golden, CO (United States)
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).
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States)
- Sponsoring Organization:
- USDOE; National Institutes of Health (NIH); National Science Foundation (NSF)
- Grant/Contract Number:
- AC02-06CH11357; HHSN272200700058C; HHSN272201200026C; CHE-1412443
- OSTI ID:
- 1764848
- Journal Information:
- Antibiotics, Vol. 9, Issue 9; ISSN 2079-6382
- Publisher:
- MDPICopyright Statement
- Country of Publication:
- United States
- Language:
- English
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