60114-64-9Relevant academic research and scientific papers
Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin
Abdelkafi, Hajer,Michau, Aurélien,Pons, Valérie,Ngadjeua, Flora,Clerget, Alexandra,Ait Ouarab, Lilia,Buisson, David-Alexandre,Montoir, David,Caramelle, Lucie,Gillet, Daniel,Barbier, Julien,Cintrat, Jean-Christophe
, p. 8114 - 8133 (2020/09/21)
High-throughput screening has shown that Retro-1 inhibits ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. To improve the activity of Retro-1, a structure-activity relationship (SAR) study was undertaken and yielded an analogue with a roughly 70-fold better half-maximal effective concentration (EC50) against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.
Thermolysis and radiofluorination of diaryliodonium salts derived from anilines
Linstad, Ethan J.,Vāvere, Amy L.,Hu, Bao,Kempinger, Jayson J.,Snyder, Scott E.,DiMagno, Stephen G.
, p. 2246 - 2252 (2017/03/17)
Aniline-derived diaryliodonium salts were synthesized and functionalized in good to excellent yields by judicious utilization of electron-withdrawing protecting groups. This simple approach opens another route to radiolabeling amino arenes in relatively complex molecules, such as flutemetamol.
Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects
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Page/Page column 43, (2008/06/13)
The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-XXI and a pharmaceutically-acceptable carrier.
ANXIOLYTIC AGENTS WITH REDUCED SEDATIVE AND ATAXIC EFFECTS
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Page/Page column 70, (2010/02/07)
Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects.
1-(2-Aminoethyl)-6-aryl-4H-triazolobenzodiazepines with Diuretic and Natriuretic Activity
Hester, Jackson B.,Ludens, James H.,Emmert, D. Edward,West, Bruce E.
, p. 1157 - 1163 (2007/10/02)
A series of 1-(2-amino-1-phenylethyl)-6-phenyl-4H-triazolobenzodiazepines was prepared and evaluated for diuretic activity.These compounds have diuretic and natriuretic activity but no kaliuretic activity when evaluated by oral administration to the conscious rat.The structure requirements for this activity are discussed.In particular it was found that the 2-aminoethyl side chain at C-1 with hydrogen or methyl substituents on the amino group was required for diuretic acitvity.A substituent at C-8 was also required: soft substituents such asmethylthio and iodo at this position favored activity.Compounds with both phenyl and 2-pyridyl substituents at C-6 were active; substituents on the C-6 phenyl, however, reduced or eliminated the activity.Substituents other than phenyl at the 1-position of the 2-aminoethyl side chain were detrimental to the activity; phenyl substitution at this position was required for activity when the substituent at C-8 was chloro but not when it was bromo.
1-Ethanamine-triazolo-benzodiazepines as diuretics
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, (2008/06/13)
Triazolo-benzodiazepine-1-ethanamines of the formulas STR1 where R, R1, R2, R3, R4 and Ring A are as defined in the specification, e.g., 8-chloro-N,N-dimethyl-β,6-diphenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiaz
