Drug-induced modifications of the immune response. 12. 4, 5-dihydro-4-oxo-2-(substituted amino)-3-furancarboxylie acids and derivatives as novel antiallergic agents

Document Type

Article

Publication Date

2-1-1988

Abstract

The synthesis of a series of novel 4, 5-dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids, salts, esters, and amides is described. The title compounds when tested in the mediator-induced dermal vascular permeability and active anaphylaxis assays in rats demonstrated moderate to potent antiallergic activity. The [2-frans-(4-methylpheny1)cyclopropyl]amino analogue 53 emerged as the most active derivative. Thus, when administered intraperitoneally to rats at a dose of 100 mg/kg, it inhibited the action of the mediators serotonin, histamine, and bradykinin by 100%. In the active anaphylaxis assay in rats, compound 30 suppressed the edema by 81% at a dose of 100 mg/kg, following intraperitoneal administration. © 1988, American Chemical Society. All rights reserved.

Publication Source (Journal or Book title)

Journal of Medicinal Chemistry

First Page

1910

Last Page

1918

This document is currently not available here.

Share

COinS