Discovery of FR115092: a novel antinephritic agent.
A series of dapsone-related 4-aminopheynl and 2-aminothiazolyl derivatives was prepared, and their antinephritic activity and blood toxicity were evaluated. 5-(2-Pyridylsulfonyl)-2-thiazolamine (FR115092, 26) was effective against two nephritis models, namely graft-versus-host disease (GVHD) and autoimmune W/BF1 mice, and showed none of the blood toxicity observed with dapsone.
Ogino
T
T
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Tsuji
K
K
Tojo
T
T
Igari
N
N
Seki
N
N
Sudo
Y
Y
Manda
T
T
Nishigaki
F
F
Matsuo
M
M
D000740:Anemia / Q000139:chemically induced; D000818:Animals; D004195:Disease Models, Animal; D008297:Male; D051379:Mice; D009393:Nephritis / Q000188:drug therapy*; D011725:Pyridines / Q000737:chemistry / Q000627:therapeutic use* / Q000633:toxicity; D013844:Thiazoles / Q000737:chemistry / Q000627:therapeutic use* / Q000633:toxicity
C116439:5-(2-pyridylsulfonyl)-2-thiazolamine; D011725:Pyridines; D013844:Thiazoles