title: Synthesis of pyrimidine derivatives possessing an antioxidative property and their inhibitory effects on picryl chloride-induced contact hypersensitivity reaction.
abstract: We conducted a preliminary structure-activity relationship (SAR) study of some barbituric acid and uracil derivatives against the picryl chloride-induced contact hypersensitivity reaction. The introduction of an antioxidative moiety to the side chain of the C(6)-position of uracil was effective against this model. The introduction of dimethoxyphenol (8b) or dimethylphenol (8c) instead of di-t-butylphenol (8a) as an antioxidative moiety gave diminished activities, so, the reactive oxygen would contribute to the inflammation of this model, and an antioxidative activity was required for exhibiting the inhibitory activity. The inhibitory activity was significantly affected by the substituent at the N(1)-phenyl moiety.
authors.affiliation: Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation, Toda, Saitama, Japan.
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Isobe
authors.forename: Kosaku
authors.initials: K
authors.lastname: Hirota
mesh_terms: D000818:Animals; D018926:Anti-Allergic Agents / Q000138:chemical synthesis / Q000627:therapeutic use; D000975:Antioxidants / Q000138:chemical synthesis* / Q000627:therapeutic use*; D003877:Dermatitis, Contact / Q000517:prevention & control*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010853:Picryl Chloride / Q000633:toxicity*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000627:therapeutic use*; D051381:Rats
chemical_list: D018926:Anti-Allergic Agents; D000975:Antioxidants; D011743:Pyrimidines; D010853:Picryl Chloride