Synthesis and evaluation of disubstituted N1- and N3-imidazolidin-2-ones acting as potential immunosuppressive agents.
New N1-mono and N1, N2-disubstituted imidazolidin-2-one with a significant immunosuppressive activity have been discovered. Among the 17 synthesized and tested compounds, five of them showed maximal inhibition of proliferation of concanavallin A (Con A)- stimulated splenocytes at 90 microM, identical to that obtained with cyclosporin A (CsA) at 5 microM, an optimal concentration.
Sabourin
Caroline
C
Laboratoire de Pharmacochimie, UPRES EA 1155, Faculté de Pharmacie, F-44035 Nantes, France.
Robert
Jean-Michel H
JM
Robert-Piessard
Sylvie
S
Carbonnelle
Delphine
D
Lang
Francois
F
D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D003208:Concanavalin A / Q000037:antagonists & inhibitors / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D005260:Female; D048289:Imidazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D013154:Spleen / Q000166:cytology / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D048289:Imidazolidines; D007166:Immunosuppressive Agents; D003208:Concanavalin A