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Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE
Antibiotics
  • Cory T Reidl, Loyola University Chicago
  • Tahirah K Heath, Loyola University Chicago
  • Iman Darwish, Loyola University Chicago
  • Rachel M Torrez, Loyola University Chicago
  • Maxwell Moore, Loyola University Chicago
  • Elliot Gild, Loyola University Chicago
  • Boguslaw P Nocek, Midwest Center for Structural Genomics and Structural Biology Center
  • Anna Starus, Loyola University Chicago
  • Richard C Holz, Colorado School of Mines
  • Daniel P Becker, Ph.D., Loyola University Chicago
Document Type
Article
Publication Date
9-11-2020
Pages
1-15
Publisher Name
MDPI
Disciplines
Abstract

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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Author Posting © The Author, 2020. This article is posted here by permission of The Authors for personal use, not for redistribution. The article was published in Antibiotics, Volume 9, Issue 9, September 2020, https://doi.org/10.3390/antibiotics9090595

Creative Commons License
Creative Commons Attribution 4.0 International
Citation Information
Cory T Reidl, Tahirah K Heath, Iman Darwish, Rachel M Torrez, et al.. "Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE" Antibiotics Vol. 9 Iss. 9 (2020)
Available at: http://works.bepress.com/daniel_p_becker/72/