Document Type
Article
Publication Date
9-11-2020
Publication Title
Antibiotics
Volume
9
Issue
9
Pages
1-15
Publisher Name
MDPI
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).
Recommended Citation
Reidl, Cory T.; Heath, Tahirah K.; Darwish, Iman; Torrez, Rachel M.; Moore, Maxwell; Gild, Elliot; Nocek, Boguslaw P.; Starus, Anna; Holz, Richard C.; and Becker, Daniel P. Ph.D.. Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE. Antibiotics, 9, 9: 1-15, 2020. Retrieved from Loyola eCommons, Chemistry: Faculty Publications and Other Works, http://dx.doi.org/10.3390/antibiotics9090595
Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 International License.
Copyright Statement
© The Author, 2020.
Comments
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