Abstract
In order to develop novel compounds for topical use possessing antiallergic as well as antiinflammatory activities, a series of o-aminophenol derivatives bearing H1-antihistaminic structures were synthesized and their effects were investigated on lipid peroxidation in rat brain homogenates, antiinflammatory effection arachidonic acid- and 12-O-tetradecanoylphorbol-13- acetate-induced mouse ear edema and antiallergic effect on 48-h homologous passive cutaneous anaphylaxis in rats. Furthermore, the effects of these compounds on delayed-type hypersensitivity reaction in mice were examined. Several N-monosubstituted amino-4-methylphenols were found to exert potent inhibitory activities in all of these assays. Of these compounds, 4m was chosen for further development as AD0261.
MeSH terms
-
Administration, Topical
-
Aminophenols / administration & dosage
-
Aminophenols / chemical synthesis
-
Aminophenols / chemistry
-
Aminophenols / pharmacology*
-
Animals
-
Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
-
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
-
Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
-
Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
-
Antioxidants / chemical synthesis
-
Antioxidants / chemistry
-
Antioxidants / pharmacology
-
Arachidonic Acid / pharmacology
-
Brain / drug effects
-
Ear
-
Edema / drug therapy
-
Guinea Pigs
-
Histamine H1 Antagonists / administration & dosage
-
Histamine H1 Antagonists / chemical synthesis
-
Histamine H1 Antagonists / pharmacology*
-
Hypersensitivity, Delayed / drug therapy*
-
Lipid Peroxidation / drug effects*
-
Male
-
Mice
-
Mice, Inbred ICR
-
Passive Cutaneous Anaphylaxis / drug effects*
-
Rats
-
Rats, Sprague-Dawley
-
Skin Tests
-
Tetradecanoylphorbol Acetate / pharmacology
Substances
-
Aminophenols
-
Anti-Inflammatory Agents, Non-Steroidal
-
Antioxidants
-
Histamine H1 Antagonists
-
2-aminophenol
-
Arachidonic Acid
-
Tetradecanoylphorbol Acetate