Quinoline-3-carbothioamides and related compounds as novel immunomodulating agents.
A series of quinoline-3-carbothioamides and their analogues was prepared via four synthetic routes and evaluated for their antinephritic and immunomodulating activities. The optimal compound 9g strongly inhibited the T-cell independent antibody production in mice immunized with TNP-LPS and was highly effective in two nephritis models, namely chronic graft-versus-host disease and autoimmune MRL/l mice.
Tojo
Takashi
T
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd, 2-1-6, Kashima,Yodogawa-ku, Osaka, Japan.
Spears
Glen W
GW
Tsuji
Kiyoshi
K
Nishimura
Hiroaki
H
Ogino
Takashi
T
Seki
Nobuo
N
Sugiyama
Aiko
A
Matsuo
Masaaki
M
D000276:Adjuvants, Immunologic / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000284:Administration, Oral; D000818:Animals; D000917:Antibody Formation / Q000187:drug effects; D001327:Autoimmune Diseases / Q000188:drug therapy; D004195:Disease Models, Animal; D004285:Dogs; D006086:Graft vs Host Disease / Q000188:drug therapy; D006207:Half-Life; D007114:Immunization; D051379:Mice; D009393:Nephritis / Q000188:drug therapy; D011507:Proteinuria / Q000188:drug therapy; D011804:Quinolines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013854:Thioamides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
D000276:Adjuvants, Immunologic; D011804:Quinolines; D013854:Thioamides; C037219:quinoline