Synthesis and immunosuppressant activity of pyrazole carboxamides.
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.
Wang
A X
AX
Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Xie
Q
Q
Lane
B
B
Mollison
K W
KW
Hsieh
G C
GC
Marsh
K
K
Sheets
M P
MP
Luly
J R
JR
Coghlan
M J
MJ
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
D007166:Immunosuppressive Agents; D007555:Isoxazoles; D011720:Pyrazoles; D000077339:Leflunomide