A series of dapsone-related 4-aminophenyl 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.