Inhibitory activities of novel pyrimidine derivatives on the contact hypersensitivity reaction.
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.
Isobe
Yoshiaki
Y
Pharmaceuticals and Biotechnology Laboratory, Japan Energy Corporation, Saitama.
Tobe
Masanori
M
Inoue
Yoshifumi
Y
Goto
Yuso
Y
Obara
Fumihiro
F
Isobe
Masakazu
M
Hayashi
Hideya
H
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
D011743:Pyrimidines