Article
Indoline-6-Sulfonamide Inhibitors of the Bacterial Enzyme DapE
Antibiotics
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).
Creative Commons License
Creative Commons Attribution 4.0 International
Copyright Statement
© The Author, 2020.
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/
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