当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Structural-activity relationship study on C-4 carbon atom of the CB1 antagonist SR141716: synthesis and pharmacological evaluation of 1,2,4-triazole-3-carboxamides.

Structural-activity relationship study on C-4 carbon atom of the CB1 antagonist SR141716: synthesis and pharmacological evaluation of 1,2,4-triazole-3-carboxamides.

Abstract：

:A series of 1,2,4-triazole-3-carboxamides has been prepared from alkyl-1,2,4-triazole-3-carboxylates under mild conditions. The ability of these triazoles to displace [3H]-CP55940 from CB1 cannabinoid receptor was measured. However, they showed only poor to moderate binding affinities, indicating that substitution of the C-4 pyrazole atom of the CB1 reference compound SR141716 by a nitrogen atom results in loss of affinity. Further investigations for functionality indicated that the compound 6a exhibited significant cannabinoid antagonistic properties in the mouse vas deferens functional assay. This leads us to the conclusion that 6a binds at a different CB1 binding site or at a new cannabinoid receptor subtype.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Jagerovic N,Hernandez-Folgado L,Alkorta I,Goya P,Martín MI,Dannert MT,Alsasua A,Frigola J,Cuberes MR,Dordal A,Holenz J

doi

10.1016/j.ejmech.2005.06.012

subject

Has Abstract

pub_date

2006-01-01 00:00:00

pages

114-20

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(05)00268-0

journal_volume

41

pub_type

杂志文章

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