title: 1,2,4-Triazolo[4,3-a]quinoxaline-1,4-diones as antiallergic agents.
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.
authors.forename: B
authors.initials: B
authors.lastname: Loev
authors.forename: J H
authors.initials: JH
authors.lastname: Musser
authors.forename: R E
authors.initials: RE
authors.lastname: Brown
authors.forename: H
authors.initials: H
authors.lastname: Jones
authors.forename: R
authors.initials: R
authors.lastname: Kahen
authors.forename: F C
authors.initials: FC
authors.lastname: Huang
authors.forename: A
authors.initials: A
authors.lastname: Khandwala
authors.forename: P
authors.initials: P
authors.lastname: Sonnino-Goldman
authors.forename: M J
authors.initials: MJ
authors.lastname: Leibowitz
mesh_terms: 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*
chemical_list: D006634:Histamine H1 Antagonists; D011810:Quinoxalines; D014230:Triazoles