Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists.
The SAR of a new series of tetrahydrocarbazole derivatives is described: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat.
Di Fabio
Romano
R
GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy. rdf26781@gsk.com
Giovannini
Riccardo
R
Bertani
Barbara
B
Borriello
Manuela
M
Bozzoli
Andrea
A
Donati
Daniele
D
Falchi
Alessandro
A
Ghirlanda
Damiano
D
Leslie
Colin P
CP
Pecunioso
Angelo
A
Rumboldt
Giovanna
G
Spada
Simone
S
D000818:Animals; D001682:Biological Availability; D016466:CHO Cells / Q000187:drug effects; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D003412:Cricetulus; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
D002227:Carbazoles; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor; C409925:1,2,3,4-tetrahydrocarbazole