1207655-27-3Relevant academic research and scientific papers
Indoline‐6‐sulfonamide inhibitors of the bacterial enzyme dape
Reidl, Cory T.,Heath, Tahirah K.,Darwish, Iman,Torrez, Rachel M.,Moore, Maxwell,Gild, Elliot,Nocek, Boguslaw P.,Starus, Anna,Holz, Richard C.,Becker, Daniel P.
, p. 1 - 15 (2020)
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).
BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
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, (2012/11/07)
The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
