Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
The synthesis and biological activity of a new series of piperazine and diazepane amides is described. The new compounds are high affinity histamine H3 ligands and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Kiev S
KS
Ly
Michael A
MA
Letavic
John M
JM
Keith
Jennifer M
JM
Miller
Emily M
EM
Stocking
Ann J
AJ
Barbier
Pascal
P
Bonaventure
Brian
B
Lord
Xiaohui
X
Jiang
Jamin D
JD
Boggs
Lisa
L
Dvorak
Kirsten L
KL
Miller
Diane
D
Nepomuceno
Sandy J
SJ
Wilson
Nicholas I
NI
Carruthers
D000577:Amides / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001381:Azepines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001921:Brain / Q000378:metabolism; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000577:Amides; D001381:Azepines; D054828:Histamine H3 Antagonists; D010879:Piperazines; D017367:Selective Serotonin Reuptake Inhibitors