title: Quinoline-3-carbothioamides and related compounds as novel immunomodulating agents.
abstract: 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.
authors.affiliation: Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd, 2-1-6, Kashima,Yodogawa-ku, Osaka, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Tojo
authors.forename: Glen W
authors.initials: GW
authors.lastname: Spears
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Tsuji
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Nishimura
authors.forename: Takashi
authors.initials: T
authors.lastname: Ogino
authors.forename: Nobuo
authors.initials: N
authors.lastname: Seki
authors.forename: Aiko
authors.initials: A
authors.lastname: Sugiyama
authors.forename: Masaaki
authors.initials: M
authors.lastname: Matsuo
mesh_terms: 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
chemical_list: D000276:Adjuvants, Immunologic; D011804:Quinolines; D013854:Thioamides; C037219:quinoline