Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake (Articolo in rivista)

Type
Label
  • Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake (Articolo in rivista) (literal)
Anno
  • 2013-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.ejmech.2012.12.056 (literal)
Alternative label
  • Manca, Ilaria; Mastinu, Andrea; Olimpieri, Francesca; Falzoi, Matteo; Sani, Monica; Ruiu, Stefania; Loriga, Giovanni; Volonterio, Alessandro; Tambaro, Simone; Bottazzi, Mirko Emilio Heiner; Zanda, Matteo; Pinna, Gerard Aime; Lazzari, Paolo (2013)
    Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake
    in European journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Manca, Ilaria; Mastinu, Andrea; Olimpieri, Francesca; Falzoi, Matteo; Sani, Monica; Ruiu, Stefania; Loriga, Giovanni; Volonterio, Alessandro; Tambaro, Simone; Bottazzi, Mirko Emilio Heiner; Zanda, Matteo; Pinna, Gerard Aime; Lazzari, Paolo (literal)
Pagina inizio
  • 256 (literal)
Pagina fine
  • 269 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 62 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 14 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Neurosci PharmaNess Sca Rl; Consiglio Nazionale delle Ricerche (CNR); Dipartimento Chim Mat & Ingn Chim Giulio Natta; Consorzio ELPRO; Dipartimento Sci Vita & Ambiente; KemoTech Srl; Consiglio Nazionale delle Ricerche (CNR); University of Aberdeen; University of Sassari (literal)
Titolo
  • Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake (literal)
Abstract
  • In spite of rimonabant's withdrawal from the European market due to its adverse effects, interest in the development of drugs based on CB1 antagonists is revamping on the basis of the peculiar properties of this class of compounds. In particular, new strategies have been proposed for the treatment of obesity and/or related risk factors through CB1, antagonists, i.e. by the development of selectively peripherally acting agents or by the identification of neutral CB1 antagonists. New compounds based on the lead 031 antagonist/inverse agonist rimonabant have been synthesized with focus on obtaining neutral CB1 antagonists. Amongst the new derivatives described in this paper, the mixture of the two enantiomers (+/-)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-(2-cyclohexyl-1-hydroxyethyl)-4-methyl-1H-pyrazole ((+/-)-5), and compound 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-[(4-2-cyclohexyl-1-fluorovinyl]-4-methyl-1H-pyrazole ((Z)-6), showed interesting pharmacological profiles. According to the preliminary pharmacological evaluation, these novel pyrazole derivatives showed in fact both neutral CB1 antagonism behaviour and significant in vivo activity towards food intake. (C) 2013 Elsevier Masson SAS. All rights reserved. (literal)
Prodotto di
Autore CNR
Insieme di parole chiave

Incoming links:


Autore CNR di
Prodotto
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi
Insieme di parole chiave di
data.CNR.it