Document Type

Article

Publication Date

9-11-2020

Publication Title

Antibiotics

Volume

9

Issue

9

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).

Comments

Author Posting © The Authors, 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 License
This work is licensed under a Creative Commons Attribution 4.0 License.

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