title: Inhibitory activities of novel pyrimidine derivatives on the contact hypersensitivity reaction.
abstract: In order to obtain novel topically applied anti-inflammatory compounds containing an inexpensive anti-oxidative moiety without chirality, we synthesized compound 2c derivatives having a di-tert-butylphenol moiety, and evaluated by topical administration their anti-inflammatory potentials on picryl chloride-(PC) induced contact hypersensitivity reaction (CHR) in mice. In the course of our structure-activity relationship (SAR) studies on the pyrimidine or the anti-oxidative moiety and the linker between them, the most potent compounds (10, 11) were obtained by the insertion of a C2 unit in compound 2c. The potencies of these compounds were 2-fold greater than that of 1. Compounds 10 and 11 were considered to be useful lead compounds having inexpensive anti-oxidative moieties without chirality.
authors.affiliation: Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation, Saitama.
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Isobe
authors.forename: Masanori
authors.initials: M
authors.lastname: Tobe
authors.forename: Yoshifumi
authors.initials: Y
authors.lastname: Inoue
authors.forename: Yuso
authors.initials: Y
authors.lastname: Goto
authors.forename: Fumihiro
authors.initials: F
authors.lastname: Obara
authors.forename: Masakazu
authors.initials: M
authors.lastname: Isobe
authors.forename: Hideya
authors.initials: H
authors.lastname: Hayashi
mesh_terms: D000287:Administration, Topical; D000818:Animals; D003877:Dermatitis, Contact / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011743:Pyrimidines / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D011743:Pyrimidines