97423-32-0

Upstream product

• 598-21-0 2-Bromoacetyl bromide 
• 51073-69-9 (2-amino-5-iodophenyl)(phenyl)methanone 
• 636-98-6 p-nitrobenzene iodide 
• 140-29-4 phenylacetonitrile 
• 2835-77-0 (2-aminophenyl)(phenyl)methanone 
• 100675-76-1 5-iodo-3-phenyl-2.1-benzoisoxazole 

Downstream Products

• 60114-64-9 7-iodo-5-phenyl-1,3-dihydro-2H-benzo[e][1,4]diazepin-2-one 
• 97423-34-2 8-Iodo-6-phenyl-1-(phenylmethyl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine 
• 97423-33-1 1,3-dihydro-7-iodo-5-phenyl-2H-1,4-benzodiazepine-2-thione 

Relevant academic research and scientific papers

Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin

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.

1-(2-Aminoethyl)-6-aryl-4H-triazolobenzodiazepines with Diuretic and Natriuretic Activity

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.