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1,2,4-Triazolo[4,3-a]quinoxaline-1,4-diones as antiallergic agents
Journal of Medicinal Chemistry1985Vol. 28(3), pp. 363–366
Citations Over TimeTop 21% of 1985 papers
Bernard Loev, JOHN H. MUSSER, Richard E. Brown, Howard Jones, Robert Kahen, Fu Chih Huang, Atul Khandwala, P. SONNINO‐GOLDMAN, Mitchell Leibowitz
Abstract
A series of new 1,4-dihydro-1,2,4-triazolo[4,3-]quinoxaline-1,4-diones has been prepared. 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 (1x), with an I50 value of 0.1 microM, is 30 times more potent than disodium cromoglycate (DSCG) in the RMC assay.
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