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3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands.

Abstract：

:A series of 3-substituted [1,2,4]triazino[4,3-c]benzimidazoles V were prepared and tested at the central benzodiazepine receptor (BzR). These compounds were designed as rigid analogues of the previously described N-benzylindolylglyoxylylamide derivatives IV. The title compounds V showed an affinity which depended directly on the presence of the N(10)-H group and an aromatic ring at position 3. Some of them elicited a 2- or 3-fold higher affinity with respect to that of the indolylglyoxylylamide derivatives IV (R = H). The GABA ratio and [(35)S]-tert-butylcyclophosphorothionate binding data revealed an efficacy profile of partial inverse agonists/antagonists for compounds 1c,e,f,j,k, and of a partial agonist for 2c. This last compound proved to be effective in antagonizing pentylenetetrazole-induced seizures in mice. Attempts were made to interpret the structure-affinity relationships of compounds V in the light of possible tautomeric equilibria involving the ligands.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Primofiore G,Da Settimo F,Taliani S,Marini AM,La Motta C,Novellino E,Greco G,Gesi M,Trincavelli L,Martini C

doi

10.1021/jm991131h

keywords:

subject

Has Abstract

pub_date

2000-01-13 00:00:00

pages

96-102

issue

1

eissn

0022-2623

issn

1520-4804

pii

jm991131h

journal_volume

43

pub_type

杂志文章

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