42779-56-6Relevant articles and documents
Small molecule inhibitors of anthrax edema factor
Jiao, Guan-Sheng,Kim, Seongjin,Moayeri, Mahtab,Thai, April,Cregar-Hernandez, Lynne,McKasson, Linda,O'Malley, Sean,Leppla, Stephen H.,Johnson, Alan T.
supporting information, p. 134 - 139 (2017/12/06)
Anthrax is a highly lethal disease caused by the Gram-(+) bacteria Bacillus anthracis. Edema toxin (ET) is a major contributor to the pathogenesis of disease in humans exposed to B. anthracis. ET is a bipartite toxin composed of two proteins secreted by the vegetative bacteria, edema factor (EF) and protective antigen (PA). Our work towards identifying a small molecule inhibitor of anthrax edema factor is the subject of this letter. First we demonstrate that the small molecule probe 5′-Fluorosulfonylbenzoyl 5′-adenosine (FSBA) reacts irreversibly with EF and blocks enzymatic activity. We then show that the adenosine portion of FSBA can be replaced to provide more drug-like molecules which are up to 1000-fold more potent against EF relative to FSBA, display low cross reactivity when tested against a panel of kinases, and are nanomolar inhibitors of EF in a cell-based assay of cAMP production.
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: Mapping of the receptor binding pocket by in silico docking studies
Di Fabio, Romano,Arban, Roberto,Bernasconi, Giovanni,Braggio, Simone,Blaney, Frank E.,Capelli, Anna M.,Castiglioni, Emiliano,Donati, Daniele,Fazzolari, Elettra,Ratti, Emiliangelo,Feriani, Aldo,Contini, Stefania,Gentile, Gabriella,Ghirlanda, Damiano,Sabbatini, Fabio M.,Andreotti, Daniele,Spada, Simone,Marchioro, Carla,Worby, Angela,St-Denis, Yves
experimental part, p. 7273 - 7286 (2009/11/30)
In an effort to discover novel CRF-1 receptor antagonists exhibiting improved physicochemical properties, a dihydropirrole[2,3]pyridine scaffold was designed and explored in terms of the SAR of the substitution at the pendent phenyl ring and the nature of
Pyridylthio-acylanilide herbicides
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, (2008/06/13)
Novel herbicidally active pyridylthio-acylanilides of the formula STR1 in which R1, R2 and R3, independently of one another, represent hydrogen, halogen, cyano or trifluoromethyl or alkyl, alkoxy and alkylthio having 1 to 4 carbon atoms in each case, R4 represents halogen, methyl or methoxy, n represents a number 0, 1 or 2, z represents the group (Ia) STR2 or the group (Ib) STR3 where X represents oxygen, sulphur, an N--R10 or N--O--R11 group, or X and Rg tpgether represent the STR4 radical, and the other radicals can have various meanings. Intermediates of the formulae STR5 are also new.