- Indoline‐6‐sulfonamide inhibitors of the bacterial enzyme dape
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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).
- 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.
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- INDOLINE SULFONAMIDE INHIBITORS OF DAPE AND NDM-1 AND USE OF THE SAME
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Indoline sulfonamide compounds that can inhibit DapE and/or bacterial metallo-β- lactamases (MBLs), such as NDM-1, are disclosed. Also disclosed are methods of treating an individual suffering from a bacterial infection using the indoline sulfonamide compounds disclosed herein.
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- INDOLINYL-SULFONAMIDE INHIBITORS OF TANKYRASE AND METHODS OF USE THEREOF
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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.
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Page/Page column 54; 55
(2016/11/21)
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- BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
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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.
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Page/Page column 132
(2012/11/07)
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- One-pot synthesis of triazolothiadiazepine 1,1-dioxide derivatives via copper-catalyzed tandem [3+2] cycloaddition/N-arylation
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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.
- Barange, Deepak Kumar,Tu, Yu-Chen,Kavala, Veerababurao,Kuo, Chun-Wei,Yao, Ching-Fa
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- ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
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This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.
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Page/Page column 41
(2009/10/22)
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- IMIDAZOLE DERIVATIVES AS FUNCTIONALLY SELECTIVE ALPHA2C ADRENORECEPTOR AGONISTS
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In its many embodiments, the present invention provides imidazole derivatives which are inhibitors of alPha2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition or amelioration of one or more conditions associated with the alpha2C adrenergic receptors using such compounds or pharmaceutical compositions. Formula (I).
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Page/Page column 40
(2008/06/13)
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- Regioselectivity of Electrophilic Aromatic Substitution: Syntheses of 6- and 7-Sulfamoylindolines and -indoles
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The previously reported chlorosulfonation of 1-acetyl-5-bromoindoline at the 7-position is in error.In actuality, the 6-substituted product is the sole regioisomer produced.This regiochemical assignment is based on NMR data and confirmed by X-ray analysis.We have prepared the first 7-sulfamoylindoline and the corresponding indole from indoline using the indoline nitrogen to direct sulfamoylation intarmolecularly to the 7-position.The new 7-substituted derivatives may prove to be important as intermediates to indole-based dyes and as herbicides.
- Borror, Alan L.,Chinoporos, Efthimios,Filosa, Michael P.,Herchen, Stephen R.,Petersen, Cheryl Pizzo,Stern, Carol A.
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p. 2047 - 2052
(2007/10/02)
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- Color transfer photographic processes and products with indole phthalein filter dyes
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This invention relates to diffusion transfer photographic processes adapted to be performed in the presence of ambient light and to diffusion transfer products useful in such processes wherein enhanced opacification particularly, in the green region of the visible spectrum is achieved by employing a 7-sulfonamido/5- or 6-sulfamoyl indole phthalein as the light-absorbing, pH-sensitive optical filter agent for the shorter wavelength region of the visible spectrum.
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