title: Synthesis and immunosuppressant activity of pyrazole carboxamides.
abstract: A series of novel pyrazole carboxamides is disclosed that demonstrate strong immunosuppressant activity in rodent and human mixed leukocyte response (MLR) assays (IC50 < 1 microM). The synthesis, biological activity, mode of action, and pharmacokinetic properties of this new lead series are discussed.
authors.affiliation: Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
authors.forename: A X
authors.initials: AX
authors.lastname: Wang
authors.forename: Q
authors.initials: Q
authors.lastname: Xie
authors.forename: B
authors.initials: B
authors.lastname: Lane
authors.forename: K W
authors.initials: KW
authors.lastname: Mollison
authors.forename: G C
authors.initials: GC
authors.lastname: Hsieh
authors.forename: K
authors.initials: K
authors.lastname: Marsh
authors.forename: M P
authors.initials: MP
authors.lastname: Sheets
authors.forename: J R
authors.initials: JR
authors.lastname: Luly
authors.forename: M J
authors.initials: MJ
authors.lastname: Coghlan
mesh_terms: D000818:Animals; D001682:Biological Availability; D006801:Humans; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007555:Isoxazoles / Q000494:pharmacology; D000077339:Leflunomide; D008213:Lymphocyte Activation / Q000187:drug effects; D007959:Lymphocyte Culture Test, Mixed; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects / Q000276:immunology
chemical_list: D007166:Immunosuppressive Agents; D007555:Isoxazoles; D011720:Pyrazoles; D000077339:Leflunomide