107144-42-3Relevant articles and documents
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 (2020/09/18)
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).
INDOLINYL-SULFONAMIDE INHIBITORS OF TANKYRASE AND METHODS OF USE THEREOF
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Page/Page column 54; 55, (2016/11/21)
The present disclosure provides compounds that may be useful for inhibiting the Tankyrase enzyme. In some aspects, these compounds are useful in the treatment of a disease or disorder related to the misregulation of Tankyrase enzyme such as cancer, degenerative diseases, or fibrotic diseases. Also provided herein are compounds may also be used to prevent the elongation of the telomere in a cell.
One-pot synthesis of triazolothiadiazepine 1,1-dioxide derivatives via copper-catalyzed tandem [3+2] cycloaddition/N-arylation
Barange, Deepak Kumar,Tu, Yu-Chen,Kavala, Veerababurao,Kuo, Chun-Wei,Yao, Ching-Fa
, p. 41 - 48 (2011/03/22)
A practical and efficient synthesis of triazolothiadiazepine-1,1-dioxide derivatives via copper-catalyzed [3+2]cycloaddition, followed by N-arylation is described. The method is also applicable to the synthesis of indoline- and thiophene-fused triazolothiadiazepine 1,1-dioxide derivatives.