Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1 H-pyrrolo[1,2- c]imidazol-1-ones: A new class of Neuropeptide S antagonists

A new lead series was identified in the NPS antagonist field. The compound was prepared following up experimental observations rationalized with computational chemistry techniques and rational design. A new class of selective NPS antagonist was developed starting from a commercially available produc...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 24; pp. 7308 - 7311
Main Authors Micheli, Fabrizio, Di Fabio, Romano, Giacometti, Angelo, Roth, Adelheid, Moro, Elisa, Merlo, Giancarlo, Paio, Alfredo, Merlo-Pich, Emilio, Tomelleri, Silvia, Tonelli, Federica, Zarantonello, Paola, Zonzini, Laura, Capelli, Anna Maria
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 2010
Subjects
Antagonist
GPR154
Neuropeptide S
NPS
NPS
GPR154
Neuropeptide S
Antagonist
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Summary:A new lead series was identified in the NPS antagonist field. The compound was prepared following up experimental observations rationalized with computational chemistry techniques and rational design. 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-1 H-pyrrolo[1,2- c]imidazol-1-one represents a new lead compound in the NPS antagonist field.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.10.067