Synthesis of various analog derivatives of ORG13514 as 5-HT1A ligands.
In connection with the development of new potential 5-HT1A ligands, multistep synthesis of N-substituted-3-aminomethyl-2,3-dihydro-1,4-dioxinol[2,3-b]pyridin e derivatives as ORG13514 analogs are described. Their biological activity as 5-HT1A type ligands is reported and compared with ORG13514 affinity and selectivity for 5-HT1A receptors.
Comoy
C
C
Institut de Chimie Organique et Analytique, associé CNRS, Université d'Orléans, France. c.comoy@meseb.u-nancy.fr
Benarab
A
A
Leinot
M
M
Monteil
A
A
Guillaumet
G
G
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D004147:Dioxins / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D004569:Electroencephalography; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D018490:Serotonin Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D012890:Sleep / Q000502:physiology; D013057:Spectrum Analysis; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D014851:Wakefulness / Q000502:physiology
D004147:Dioxins; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D018490:Serotonin Agents; D013141:Spiro Compounds