Synthesis and immunosuppressive activity evaluation of substituted N-imidazolidin-2-ones and N-tetrahydropyrimidin-2(1H)-ones.
Seventeen compounds with either an imidazolin-2-one or a tetrahydropyrimidin-2(1H)-one scaffold were synthesized and evaluated for their immunosuppressive activity in a concanavallin A (ConA)-stimulated mouse splenocytes proliferation test. Three of these molecules exerted a significant activity at 90 microM. All the compounds of the tetrahydropyrimidin-2(1H)-one series have turned out to be inactive showing the crucial role of the imidazolidin-2-one scaffold in the induction of an immunosuppressive activity.
Sabourin
Caroline
C
Departement de Pharmacochimie, Faculté de Pharmacie, Université de Nantes, Nantes, France. caroline.sabourin@univ-nantes.fr
Robert
Jean-Michel
JM
D000818:Animals; D049109:Cell Proliferation; D003208:Concanavalin A / Q000494:pharmacology; D048289:Imidazolidines / Q000138:chemical synthesis / Q000494:pharmacology*; D007166:Immunosuppressive Agents / Q000138:chemical synthesis*; D051379:Mice; D008810:Mice, Inbred C57BL; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000494:pharmacology*; D013154:Spleen / Q000166:cytology; D013329:Structure-Activity Relationship
D048289:Imidazolidines; D007166:Immunosuppressive Agents; D011744:Pyrimidinones; C505709:tetrahydropyrimidinone; D003208:Concanavalin A