Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: a new class of Neuropeptide S antagonists.
A new class of selective NPS antagonist was developed starting from a commercially available product identified by screening activities. Experimental NMR observations and computational experiments allowed the discovery of a new class of derivatives. 5-Phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-one represents a new lead compound in the NPS antagonist field.
Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Verona, Italy. fabrizio.micheli@aptuit.com
Fabrizio
F
Micheli
Romano
R
Di Fabio
Angelo
A
Giacometti
Adelheid
A
Roth
Elisa
E
Moro
Giancarlo
G
Merlo
Alfredo
A
Paio
Emilio
E
Merlo-Pich
Silvia
S
Tomelleri
Federica
F
Tonelli
Paola
P
Zarantonello
Laura
L
Zonzini
Anna Maria
AM
Capelli
D000818:Animals; D053961:Azabicyclo Compounds / Q000737:chemistry*; D003198:Computer Simulation; D015195:Drug Design; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008862:Microsomes, Liver / Q000378:metabolism; D009479:Neuropeptides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010880:Piperidines / Q000737:chemistry*; D051381:Rats; D013816:Thermodynamics
D053961:Azabicyclo Compounds; D007093:Imidazoles; D009479:Neuropeptides; D010880:Piperidines; C506531:neuropeptide S, human