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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Synthesis and topical antiinflammatory and antiallergic activities of antioxidant o-aminophenol derivatives.

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.[1]

References

  1. Synthesis and topical antiinflammatory and antiallergic activities of antioxidant o-aminophenol derivatives. Sugiyama, N., Akahoshi, F., Kuwahara, S., Kajii, M., Sakaue, Y., Yakumaru, H., Sugiura, M., Fukaya, C. J. Med. Chem. (1994) [Pubmed]
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