1,2,4-Triazolo[4,3-a]quinoxaline-1,4-diones as antiallergic agents.
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.
Loev
B
B
Musser
J H
JH
Brown
R E
RE
Jones
H
H
Kahen
R
R
Huang
F C
FC
Khandwala
A
A
Sonnino-Goldman
P
P
Leibowitz
M J
MJ
D000818:Animals; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects; D006967:Hypersensitivity / Q000188:drug therapy*; D008297:Male; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D011810:Quinoxalines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*
D006634:Histamine H1 Antagonists; D011810:Quinoxalines; D014230:Triazoles