Jung, Michael E. published the artcileStructure-Activity Relationship of Semicarbazone EGA Furnishes Photoaffinity Inhibitors of Anthrax Toxin Cellular Entry, COA of Formula: C8H4ClF3O, the main research area is phenyl azide photoaffinity inhibitor anthrax toxin semicarbazone EGA SAR; Photoaffinity labeling; anthrax lethal toxin; aryl azide; endosomal trafficking; semicarbazone.
[In this abstract compounds 1-5 are represented by graphic structure I as follows: 1: X, Y = H, Z = Br; 2: X = F, Y = H, Z = Br; 3: X = F, Y = H, Z = N3; 4: X, Y = H, Z = N3; 5: X, Y = F, Z = N3]. EGA, 1, prevents the entry of multiple viruses and bacterial toxins into mammalian cells by inhibiting vesicular trafficking. The cellular target of 1 is unknown, and a structure-activity relationship study was conducted in order to develop a strategy for target identification. A compound with mid-nanomolar potency was identified (2), and three photoaffinity labels were synthesized (3-5). For this series, the expected photochem. of the Ph azide moiety is a more important factor than the IC50 of the photoprobe in obtaining a successful photolabeling event. While 3 was the most effective reversible inhibitor of the series, it provided no protection to cells against anthrax lethal toxin (LT) following UV irradiation Conversely, 5, which possessed weak bioactivity in the standard assay, conferred robust irreversible protection vs LT to cells upon UV photolysis.
ACS Medicinal Chemistry Letters published new progress about Alkylation, regioselective (of semicarbazone core). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, COA of Formula: C8H4ClF3O.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics