Document Detail


Novel pyrazole derivatives as neutral CB(1) antagonists with significant activity towards food intake.
MedLine Citation:
PMID:  23357307     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
In spite of rimonabant's withdrawal from the European market due to its adverse effects, interest in the development of drugs based on CB(1) 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 CB(1) antagonists, i.e. by the development of selectively peripherally acting agents or by the identification of neutral CB(1) antagonists. New compounds based on the lead CB(1) antagonist/inverse agonist rimonabant have been synthesized with focus on obtaining neutral CB(1) 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-[(Z)-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 CB(1) antagonism behaviour and significant in vivo activity towards food intake.
Authors:
Ilaria Manca; Andrea Mastinu; Francesca Olimpieri; Matteo Falzoi; Monica Sani; Stefania Ruiu; Giovanni Loriga; Alessandro Volonterio; Simone Tambaro; Mirko Emilio Heiner Bottazzi; Matteo Zanda; Gérard Aimè Pinna; Paolo Lazzari
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-11
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  62C     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  256-269     Citation Subset:  -    
Copyright Information:
Copyright © 2013 Elsevier Masson SAS. All rights reserved.
Affiliation:
Neuroscienze PharmaNess S.c.a r.l., Edificio 5, Loc. Piscinamanna, 09010 Pula (CA), Italy.
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