Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.
Following the program started at Johnson & Johnson Pharmaceutical Research & Development searching for 5-HT(2A/2C) antagonists we now report on the synthesis of a series of substituted 2-(aminomethyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives. The 5-HT2A, 5-HT2C and H1 receptor affinities of the described compounds are reported. The mCCP antagonistic activity of a set of selected molecules is also reported.
Cid
José
J
Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen-Cilag, Medicinal Chemistry Department, Jarama s/n, 45007 Toledo, Spain. jcid@prdes.jnj.com
Alonso
José M
JM
Andrés
José I
JI
Fernández
Javier
J
Gil
Pilar
P
Iturrino
Laura
L
Matesanz
Encarna
E
Meert
Theo F
TF
Megens
Anton
A
Sipido
Victor K
VK
Trabanco
Andrés A
AA
D005663:Furans / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D011869:Radioligand Assay; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D005663:Furans; D008024:Ligands; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists