
Journal of Medicinal Chemistry p. 363 - 366 (1985)
Update date:2022-08-05
Topics:
Loev
Musser
Brown
Jones
Kahen
Huang
Khandwala
Sonnino-Goldman
Leibowitz
A series of new 1,4-dihydro-1,2,4-triazolo[4,3-a]quinoxaline-1,4-diones has been reported. These compounds were tested as inhibitors of antigen-induced release of histamine (AIR) in vitro from rat peritoneal mast cells (RMC) and as inhibitors of IgE-mediated rat passive cutaneous anaphylaxis (PCA). Most of this new class of antiallergic agents showed good activity in the RMC and PCA tests. The most potent compound, 2-acetyl-7-chloro-5-n-propyl-1,2,4-triazolo[4,3-a]quinoxaline-1,4-dione, with an I50 value of 0.1 μM, is 30 times more potent than disodium cromoglycate (DSCG) in the RMC assay.
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